subject:(Receptors)

University of North Carolina – Greensboro

1. Singh, Jagjeet. A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein.

Degree: 2014, University of North Carolina – Greensboro

URL: http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=16606

► One key signaling pathway in the cellular signaling involving G protein coupled receptors (GPCR) is via heterotrimeric G proteins. The first step in GPCR/G protein… (more)

▼ One key signaling pathway in the cellular signaling involving G protein coupled receptors (GPCR) is via heterotrimeric G proteins. The first step in GPCR/G protein signaling is the activation of a GPCR by the ligand binding and the next step is the activation of the G protein. Understanding the molecular mechanism behind the GPCR/G protein interactions will help in characterizing this important signaling pathway and should ultimately lead to the design of functionally selective ligands for this larger class of receptors. Earlier, the Reggio group used molecular dynamics simulations to study the activation of the cannabinoid CB2 receptor, a class A GPCR, by its endogenous ligand, 2-arachidonoylglycerol (2-AG) via the lipid bilayer. The goal of the current project was to study the next step in the G-protein mediated signal transduction, when an agonist activated CB2 receptor forms a complex with Gi protein and catalyzes the activation of Gi protein, releasing the guanosine diphosphate (GDP) bound between the ras-like (also known as GTPase domain) and helical domains of the Gá protein. To this end, we report here the CB2 / Gái1â1ã2 complex formation using our 2-AG activated CB2 receptor model. For G protein activation (dissociation of GDP), we hypothesized that GDP release from the ras-like and helical domains of Gái would be triggered by the hydration of GDP. We probed the role of the CB2 receptor interactions with the Gái protein and the resultant progression of GDP hydration. We have seen the number of waters surrounding GDP increase from 16 (t= 0 ns) to 28 waters (t=5 ìs). Two important interactions between the receptor and G-protein appear to lead to the increased hydration of GDP. (1) A hydrophobic interaction occurred between CB2 IC2 loop residue P139 and the Gái hydrophobic pocket residues: V34 (N terminus; L194 (â1 sheet); F196 (â2 sheet); and, F336, T340, I343, I344 (á5 helix) multiple times in our 5 ìs long trajectory. Each time this interaction occurred, an increase in GDP hydration was observed in our simulation. 2) We also observed an IC3 loop interaction with the Gái á4 helix between 1.4 to 1.6 ìs, in which the IC3 loop residue R229 reached to interact with E297 and E298. Taken together, our results show that the intracellular loops play a critical role in the hydration of GDP that should lead to G protein activation.; Cellular signaling, Cannabinoid CB2 receptor Advisors/Committee Members: Patricia Reggio (advisor).

Subjects/Keywords: G proteins – Receptors; Cannabinoids – Receptors

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APA (6^th Edition):

Singh, J. (2014). A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein. (Doctoral Dissertation). University of North Carolina – Greensboro. Retrieved from http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=16606

Chicago Manual of Style (16^th Edition):

Singh, Jagjeet. “A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein.” 2014. Doctoral Dissertation, University of North Carolina – Greensboro. Accessed March 02, 2021. http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=16606.

MLA Handbook (7^th Edition):

Singh, Jagjeet. “A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein.” 2014. Web. 02 Mar 2021.

Vancouver:

Singh J. A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein. [Internet] [Doctoral dissertation]. University of North Carolina – Greensboro; 2014. [cited 2021 Mar 02]. Available from: http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=16606.

Council of Science Editors:

Singh J. A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein. [Doctoral Dissertation]. University of North Carolina – Greensboro; 2014. Available from: http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=16606

University of Waterloo

2. Sethi, Neha. The interaction of chemicals isolated from municipal wastewater effluent with rainbow trout (Oncorhynchus mykiss) thyroid hormone receptors.

Degree: 2012, University of Waterloo

URL: http://hdl.handle.net/10012/7126

► The normal function of the thyroid hormone (TH) system is essential for growth, development and metabolism in humans as well as in other species. The… (more)

▼ The normal function of the thyroid hormone (TH) system is essential for growth, development and metabolism in humans as well as in other species. The action of TH is dependent on its binding to thyroid hormone receptors (THR) found in the cell nucleus. In some situations, chemicals with structural similarities to TH can bind to these receptors and disrupt their normal function. It has been previously demonstrated that environmental contaminants including, carbamazapine, nonlyphenol (NP), bisphenol A (BPA), and several others are able to bind to the THR as either agonists or antagonists and modulate downstream biochemical responses. Municipal wastewater effluent (MWWE) is a major source of these contaminants entering aquatic environments. Recently extracts of MWWE have been shown to contain chemicals that are capable of binding to THRs. However, MWWE is a complex mixture of chemicals and the specific chemicals have not been identified. In this thesis, a proof of concept was developed for using an Effects Directed Assessment (EDA) approach to isolate thyroid receptor active compounds in MWWE. An EDA is a technique created to extract and identify chemicals from complex mixtures, using various fractionation methods. Once these chemicals have been identified, they are further reviewed for biological relevance. A competitive binding assay for THR was developed and applied to determine the relative binding affinity of known environmental contaminants to THR. Nuclear thyroid hormone receptors were isolated from rainbow trout liver by differential centrifugation. This method involved liver tissue homogenization and subsequent centrifugations to separate the nuclear fraction containing the receptors. The binding characteristics of the isolated THR were evaluated using the thyroid hormones triiodothyronine (T3) and thyroxine (T4) in a competitive binding assay. Minimal binding affinity was present in this assay and future studies should validate the assay further and assure that it is comparable to literature values. Environmental contaminants, including BPA, NP were also tested to determine their relative binding affinity to the THRs compared to the endogenous hormones. High concentrations of both BPA and NP bound to the thyroid hormone receptor, displacing radiolabeled T3 from its binding site. The rainbow trout competitive binding assay was also used to test the binding affinities of extracts from two municipal wastewater effluents collected in the Grand River watershed in southern Ontario. Effluents were extracted using a solid phase adsorbent (HLB Oasis cartridge), eluted with methanol, taken to dryness then reconstituted in ethanol for use in the assay. Both effluent extracts displaced the binding of radiolabeled T3 to the thyroid receptors. The studies demonstrate that a competitive THR assay can be used to detect chemicals in complex mixtures with the potential to interact with THRs. The next step should be to apply the assay using an EDA approach to isolate and identify specific chemicals in effluents that are…

Subjects/Keywords: Thyroid; Receptors

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APA (6^th Edition):

Sethi, N. (2012). The interaction of chemicals isolated from municipal wastewater effluent with rainbow trout (Oncorhynchus mykiss) thyroid hormone receptors. (Thesis). University of Waterloo. Retrieved from http://hdl.handle.net/10012/7126

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Sethi, Neha. “The interaction of chemicals isolated from municipal wastewater effluent with rainbow trout (Oncorhynchus mykiss) thyroid hormone receptors.” 2012. Thesis, University of Waterloo. Accessed March 02, 2021. http://hdl.handle.net/10012/7126.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Sethi, Neha. “The interaction of chemicals isolated from municipal wastewater effluent with rainbow trout (Oncorhynchus mykiss) thyroid hormone receptors.” 2012. Web. 02 Mar 2021.

Vancouver:

Sethi N. The interaction of chemicals isolated from municipal wastewater effluent with rainbow trout (Oncorhynchus mykiss) thyroid hormone receptors. [Internet] [Thesis]. University of Waterloo; 2012. [cited 2021 Mar 02]. Available from: http://hdl.handle.net/10012/7126.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Sethi N. The interaction of chemicals isolated from municipal wastewater effluent with rainbow trout (Oncorhynchus mykiss) thyroid hormone receptors. [Thesis]. University of Waterloo; 2012. Available from: http://hdl.handle.net/10012/7126

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Rutgers University

3. Halikere, Apoorva, 1989-. Synaptic mechanisms of OPRM1 A118G single nucleotide polymorphism in human neurons.

Degree: PhD, Neuroscience, 2018, Rutgers University

URL: https://rucore.libraries.rutgers.edu/rutgers-lib/57584/

►

Association of the non-synonymous single nucleotide polymorphism (SNP) rs1799971 in OPRM1 to drug dependence and alcohol abuse suggests it may have a functional consequence in… (more)

▼

Association of the non-synonymous single nucleotide polymorphism (SNP) rs1799971 in OPRM1 to drug dependence and alcohol abuse suggests it may have a functional consequence in altering receptor signaling in the brain. The A118G SNP causes a switch of asparagine (N) at position 40 of the mu-opioid receptor (MOR) to aspartate (D). To dissect the underlying neural and synaptic basis of the N40D MOR variant, we generated human GABAergic induced neuronal (iN) cells from induced pluripotent stem (iPS) cells of donors homozygous for either the major (N40) or minor (D40) alleles of the MOR. We found that the subject-derived iN cells exhibit mature neuronal properties such as action potential firing and neuronal excitability and express functional MORs. Interestingly, upon MOR activation by the agonist DAMGO, D40 MOR iN cells exhibit consistently stronger suppression of spontaneous inhibitory postsynaptic currents (sIPSCs) than N40 MOR iN cells across multiple subjects. To mitigate the complexity of diverse genetic backgrounds of the subject iN cells derived from multiple human subjects, we employed CRISPR/Cas9 genome-editing to generate two pairs of isogenic human pluripotent stem cell lines. Remarkably, the synaptic regulation of MOR activation in the isogenic lines recapitulate those of neurons generated from different individuals, i.e. stronger suppression in D40 MOR carrying human neuronal cells by MOR activation. We further determined that the increased sensitivity of D40 iN cells to DAMGO was caused by a more robust inhibition of excitability and synaptic release by DAMGO in D40 MOR expressing neurons. Additionally, we found that the N40D SNP influences the development of long-term tolerance at the MOR. Specifically, D40 iN cells are unable to develop adaptive changes in synaptic function unlike N40 iN cells following long-term mu opioid receptor activation by DAMGO. This study utilizes patient-specific iPS cells as well as a gene edited isogenic neurons to advance our understanding of the fundamental synaptic alterations associated with OPRM1 A118G in a human neuronal context.

Advisors/Committee Members: Pang, Zhiping (chair), Pintar, John E (internal member), Hart, Ronald P (internal member), Blendy, Julie A (outside member), School of Graduate Studies.

Subjects/Keywords: Opioids – Receptors

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Halikere, Apoorva, 1. (2018). Synaptic mechanisms of OPRM1 A118G single nucleotide polymorphism in human neurons. (Doctoral Dissertation). Rutgers University. Retrieved from https://rucore.libraries.rutgers.edu/rutgers-lib/57584/

Chicago Manual of Style (16^th Edition):

Halikere, Apoorva, 1989-. “Synaptic mechanisms of OPRM1 A118G single nucleotide polymorphism in human neurons.” 2018. Doctoral Dissertation, Rutgers University. Accessed March 02, 2021. https://rucore.libraries.rutgers.edu/rutgers-lib/57584/.

MLA Handbook (7^th Edition):

Halikere, Apoorva, 1989-. “Synaptic mechanisms of OPRM1 A118G single nucleotide polymorphism in human neurons.” 2018. Web. 02 Mar 2021.

Vancouver:

Halikere, Apoorva 1. Synaptic mechanisms of OPRM1 A118G single nucleotide polymorphism in human neurons. [Internet] [Doctoral dissertation]. Rutgers University; 2018. [cited 2021 Mar 02]. Available from: https://rucore.libraries.rutgers.edu/rutgers-lib/57584/.

Council of Science Editors:

Halikere, Apoorva 1. Synaptic mechanisms of OPRM1 A118G single nucleotide polymorphism in human neurons. [Doctoral Dissertation]. Rutgers University; 2018. Available from: https://rucore.libraries.rutgers.edu/rutgers-lib/57584/

University of Alberta

4. McEown, Kristopher Scott. The Roles of Mineralocorticoid and GABAA Receptors in Anxiety and Fear Memory.

Degree: PhD, Department of Psychology, 2013, University of Alberta

URL: https://era.library.ualberta.ca/files/12579t871

► The purpose of this dissertation was to examine the roles of brain mineralocorticosteroid (MR) and γ-aminobutyric acid (GABAA) receptors in mediating unconditioned fear and fear… (more)

▼ The purpose of this dissertation was to examine the roles of brain mineralocorticosteroid (MR) and γ-aminobutyric acid (GABAA) receptors in mediating unconditioned fear and fear memory. The first set of experiments explored the role of hippocampal and medial prefrontal cortex mineralocorticosteroid receptors (MRs) in anxiety and fear memory. The MR antagonist RU28318 was microinfused into the dorsal hippocampus (DH), ventral hippocampus (VH) or medial prefrontal cortex (mPFC) ten minutes prior to testing in two rodent models of unconditioned anxiety, the elevated plus-maze and shock-probe burying test. Fear memory was then assessed in the shock-probe apparatus 24 hours later by re-exposing non-drugged rats to a non-electrified probe. RU28318 infusions into the VH reduced anxiety in the elevated plus-maze while RU28318 in the DH or mPFC did not. In contrast, RU28318 infusions into the DH, VH and mPFC all reduced anxiety in the shock-probe burying test. Fear memory was not affected by infusions into any of the three brain regions. The second set of experiments examined the role of hippocampal GABAA receptor sub-units in mediating anxiety and fear memory. α2 GABAA receptor sub-units are thought to mediate the anxiolytic effects of benzodiazepines and α5 sub-units are thought to mediate the amnesic effects of benzodiazepines. The DH and VH both contain GABAA receptors having these sub-units. Rats were given intra-hippocampal microinfusions of either TPA023 (an α2 agonist) or TB-21007 (an α5 inverse agonist) and tested in the plus-maze and shock-probe tests. Twenty-four hours later, rats were tested for fear memory with the non-electrified shock-probe. The α2 agonist (TPA023) reduced anxiety when it was infused into the VH but had no effect when infused into the DH. Conversely, the inverse α5 agonist (TB-21007) impaired fear memory when it was infused into the DH, but not when it was infused into the VH. Overall, these results suggest that mineralocorticoid and GABAA receptors in the ventral hippocampus mediate anxiety. In addition, these results suggest that ventral hippocampal GABAA α2 sub-units mediate anxiety and dorsal hippocampal GABAA α5 sub-units mediate fear memory.

Subjects/Keywords: Anxiety; Fear Memory; Mineralocorticoid Receptors; GABAA Receptors

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

McEown, K. S. (2013). The Roles of Mineralocorticoid and GABAA Receptors in Anxiety and Fear Memory. (Doctoral Dissertation). University of Alberta. Retrieved from https://era.library.ualberta.ca/files/12579t871

Chicago Manual of Style (16^th Edition):

McEown, Kristopher Scott. “The Roles of Mineralocorticoid and GABAA Receptors in Anxiety and Fear Memory.” 2013. Doctoral Dissertation, University of Alberta. Accessed March 02, 2021. https://era.library.ualberta.ca/files/12579t871.

MLA Handbook (7^th Edition):

McEown, Kristopher Scott. “The Roles of Mineralocorticoid and GABAA Receptors in Anxiety and Fear Memory.” 2013. Web. 02 Mar 2021.

Vancouver:

McEown KS. The Roles of Mineralocorticoid and GABAA Receptors in Anxiety and Fear Memory. [Internet] [Doctoral dissertation]. University of Alberta; 2013. [cited 2021 Mar 02]. Available from: https://era.library.ualberta.ca/files/12579t871.

Council of Science Editors:

McEown KS. The Roles of Mineralocorticoid and GABAA Receptors in Anxiety and Fear Memory. [Doctoral Dissertation]. University of Alberta; 2013. Available from: https://era.library.ualberta.ca/files/12579t871

University of Ottawa

5. Hristova, Elitza. Sigma-1 Receptor (σ – 1R) Activation and Modulation of NMDA Receptor Surface Expression .

Degree: 2014, University of Ottawa

URL: http://hdl.handle.net/10393/31784

► The sigma-1 receptors (σ-1Rs) are endoplasmic reticulum (ER) resident proteins shown to have chaperone-like functions, and are widely distributed throughout the central nervous system (CNS).… (more)

Subjects/Keywords: Sigma-1 receptors; NMDA receptors; Hippocampus

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APA (6^th Edition):

Hristova, E. (2014). Sigma-1 Receptor (σ – 1R) Activation and Modulation of NMDA Receptor Surface Expression . (Thesis). University of Ottawa. Retrieved from http://hdl.handle.net/10393/31784

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Hristova, Elitza. “Sigma-1 Receptor (σ – 1R) Activation and Modulation of NMDA Receptor Surface Expression .” 2014. Thesis, University of Ottawa. Accessed March 02, 2021. http://hdl.handle.net/10393/31784.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Hristova, Elitza. “Sigma-1 Receptor (σ – 1R) Activation and Modulation of NMDA Receptor Surface Expression .” 2014. Web. 02 Mar 2021.

Vancouver:

Hristova E. Sigma-1 Receptor (σ – 1R) Activation and Modulation of NMDA Receptor Surface Expression . [Internet] [Thesis]. University of Ottawa; 2014. [cited 2021 Mar 02]. Available from: http://hdl.handle.net/10393/31784.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Hristova E. Sigma-1 Receptor (σ – 1R) Activation and Modulation of NMDA Receptor Surface Expression . [Thesis]. University of Ottawa; 2014. Available from: http://hdl.handle.net/10393/31784

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Central Connecticut State University

6. Ngu, Tuong, 1988-. Hydrocortisone acting as an inhibitor of GABA receptor in the red crayfish (Procambarus clarkii) muscle receptor organ.

Degree: Department of Biological Sciences, 2016, Central Connecticut State University

URL: http://content.library.ccsu.edu/u?/ccsutheses,2360

"Submitted in Partial Fulfillment of the Requirements for the Degree of Master of Science in Biological Science with Health Specialization."; Thesis advisor: Mark Jackson.; M.S.,Central Connecticut State University,,2016.; Advisors/Committee Members: Jackson, Mark E.

Subjects/Keywords: Hydrocortisone.; GABA – Receptors.; Procambarus clarkii.; Muscle receptors.

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APA (6^th Edition):

Ngu, Tuong, 1. (2016). Hydrocortisone acting as an inhibitor of GABA receptor in the red crayfish (Procambarus clarkii) muscle receptor organ. (Thesis). Central Connecticut State University. Retrieved from http://content.library.ccsu.edu/u?/ccsutheses,2360

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Ngu, Tuong, 1988-. “Hydrocortisone acting as an inhibitor of GABA receptor in the red crayfish (Procambarus clarkii) muscle receptor organ.” 2016. Thesis, Central Connecticut State University. Accessed March 02, 2021. http://content.library.ccsu.edu/u?/ccsutheses,2360.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Ngu, Tuong, 1988-. “Hydrocortisone acting as an inhibitor of GABA receptor in the red crayfish (Procambarus clarkii) muscle receptor organ.” 2016. Web. 02 Mar 2021.

Vancouver:

Ngu, Tuong 1. Hydrocortisone acting as an inhibitor of GABA receptor in the red crayfish (Procambarus clarkii) muscle receptor organ. [Internet] [Thesis]. Central Connecticut State University; 2016. [cited 2021 Mar 02]. Available from: http://content.library.ccsu.edu/u?/ccsutheses,2360.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Ngu, Tuong 1. Hydrocortisone acting as an inhibitor of GABA receptor in the red crayfish (Procambarus clarkii) muscle receptor organ. [Thesis]. Central Connecticut State University; 2016. Available from: http://content.library.ccsu.edu/u?/ccsutheses,2360

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Hong Kong University of Science and Technology

7. He, Wei. Single-particle tracking of acetylcholine receptors and ganglioside GM1 on live cell membranes.

Degree: 2015, Hong Kong University of Science and Technology

URL: http://repository.ust.hk/ir/Record/1783.1-83591 ; https://doi.org/10.14711/thesis-b1477557 ; http://repository.ust.hk/ir/bitstream/1783.1-83591/1/th_redirect.html

► Single-particle tracking was used to monitor 2 highly expressed molecules in live Xenopus muscle cells: the transmembrane ion channel acetylcholine receptor (AChR) and the outer-leaflet… (more)

▼ Single-particle tracking was used to monitor 2 highly expressed molecules in live Xenopus muscle cells: the transmembrane ion channel acetylcholine receptor (AChR) and the outer-leaflet lipid-raft marker ganglioside GM1. AChRs and GM1s were labeled with quantum dots linked to specific toxins, and up to 200 molecules per frame were concurrently tracked at a high sampling frequency (80 Hz) and over a long duration (30 min). In untreated cells, both AChRs and GM1s diffused without marked confinement within a 6-μm range over a long period. However, their instantaneous diffusion coefficient δ was distributed over a broad range and featured an exponential tail. This dynamic heterogeneity was observed in cells under various conditions. Protein networks underneath the membrane, such as those formed by F-actin and scaffold proteins, were examined for their role in regulating the dynamic heterogeneity; for this analysis, cells were exposed to 5 drugs, and the results showed that whereas ATP depletion homogenized the heterogeneity in δ by eliminating cortical F-actin, reducing the membrane cholesterol content did not exert a major effect. By combining the findings of unconfined diffusion, a broad distribution of δ, and the drastic influence of cortical F-actin disruption, we developed a new hypothesis on membrane organization based on the picket-fence model. Moreover, here we report 2 previously unrecognized behaviors of AChRs: First, AChRs moved linearly toward HB-GAM-coated beads. Our results indicated that AChRs’ linear motion toward the beads is guided by motor proteins, rather than by a vehicle that syncs their step speed. Second, transient coalescence (TC) occurred between AChRs and between GM1s. These TC events indicate that certain immobilization sites exist on the plasma membrane that are likely generated by actin polymerization and cholesterol. The sites were frequently detected between bead-induced immobile AChRs and mobile AChRs, and they might facilitate AChR cluster formation.

Subjects/Keywords: Cell membranes ; Nicotinic receptors ; Acetylcholine ; Receptors ; Gangliosides

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

He, W. (2015). Single-particle tracking of acetylcholine receptors and ganglioside GM1 on live cell membranes. (Thesis). Hong Kong University of Science and Technology. Retrieved from http://repository.ust.hk/ir/Record/1783.1-83591 ; https://doi.org/10.14711/thesis-b1477557 ; http://repository.ust.hk/ir/bitstream/1783.1-83591/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

He, Wei. “Single-particle tracking of acetylcholine receptors and ganglioside GM1 on live cell membranes.” 2015. Thesis, Hong Kong University of Science and Technology. Accessed March 02, 2021. http://repository.ust.hk/ir/Record/1783.1-83591 ; https://doi.org/10.14711/thesis-b1477557 ; http://repository.ust.hk/ir/bitstream/1783.1-83591/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

He, Wei. “Single-particle tracking of acetylcholine receptors and ganglioside GM1 on live cell membranes.” 2015. Web. 02 Mar 2021.

Vancouver:

He W. Single-particle tracking of acetylcholine receptors and ganglioside GM1 on live cell membranes. [Internet] [Thesis]. Hong Kong University of Science and Technology; 2015. [cited 2021 Mar 02]. Available from: http://repository.ust.hk/ir/Record/1783.1-83591 ; https://doi.org/10.14711/thesis-b1477557 ; http://repository.ust.hk/ir/bitstream/1783.1-83591/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

He W. Single-particle tracking of acetylcholine receptors and ganglioside GM1 on live cell membranes. [Thesis]. Hong Kong University of Science and Technology; 2015. Available from: http://repository.ust.hk/ir/Record/1783.1-83591 ; https://doi.org/10.14711/thesis-b1477557 ; http://repository.ust.hk/ir/bitstream/1783.1-83591/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

University of North Carolina – Greensboro

8. Lingerfelt, Mary A. Construction and validation of GPR55 active and inactive state in silico models through the use of biological assays, mutation data, and structure activity relationships.

Degree: 2016, University of North Carolina – Greensboro

URL: http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=21355

► G-protein coupled receptors (GPCRs) function as both gatekeepers and molecular messengers of the cell. They relay signals that span the cell membrane mediating nearly every… (more)

▼ G-protein coupled receptors (GPCRs) function as both gatekeepers and molecular messengers of the cell. They relay signals that span the cell membrane mediating nearly every significant physiological process and currently represent the target of about 30% of all drugs. The signals they transmit can arise from a remarkable variety of stimuli which includes, but is not limited to, photons, neurotransmitters and hormones. GPR55, a rhodopsin-like (Class A) GPCR, has received a great deal of attention due to its emerging involvement in a multitude of physiological processes and its putative identity as a third type of cannabinoid receptor. Characterizations of GPR55 knock-out mice reveal a role for the receptor in controlling inflammatory pain, neuropathic pain, and bone resorption.1 Myriad other studies indicate that GPR55 activation may play a part in oncogenesis and metathesis. GPR55 can be found in numerous tissue types throughout the body and is also highly expressed throughout the cerebellum and surrounding central nervous system lending credence to the idea that this receptor may play a more crucial physiological role than originally thought.2 GPR55 has an extensive physiological profile and has been shown to respond uniquely to a great number of diverse compounds. Specifically, it has been shown to recognize many cannabinoid compounds, including CB1 and CB2 endogenous ligands, phytocannabinoids and synthetic cannabinoids. Similar to the ligands of the CB1 and CB2 receptors, the endogenous ligand of GPR55, lysophosphatidylinositol (LPI), is a lipid-derived molecule.3 LPI activates ERK1/2 and increases [Ca2+] and, to date, there has been no evidence that LPI interacts with the other cannabinoid receptors. Despite innumerable prospective clinical uses hinted at by the aforementioned research no low nanomolar potency ligands of GPR55 have been identified. Nor has there been a radio-ligand developed to characterize the binding site of this receptor. Lack of such tools is a great impediment to any forward progress towards developing the GPR55 receptor as a therapeutic target for drug design. The following research details the creation of both a GPR55 active- and a GPR55 inactive- state homology model. Towards this goal, Chapter I details the background of the discovery, pharmacological relevance and ligand scope of GPR55. Its purpose is to establish a framework for the research that follows and highlight the medical importance of this elusive receptor. Chapter II describes the synthetic preparation of antagonists of GPR55 for use in preliminary SAR studies. The original high throughput screen that lead to the identification of novel GPR55 scaffold chemotypes from the screening of over 300,000 compounds gave rise to the piperidinyloxadiazolone compound CID23612552 and the synthetic diversification of what was then dubbed Scaffold 1. A detailed description of the methods used in the construction of the updated R and R* state of GPR55 models is handled in Chapter III. A combination of Conformational Memories4,5 (using the… Advisors/Committee Members: Patricia Reggio (advisor).

Subjects/Keywords: G proteins – Receptors; Cannabinoids – Receptors; Ligands (Biochemistry)

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APA (6^th Edition):

Lingerfelt, M. A. (2016). Construction and validation of GPR55 active and inactive state in silico models through the use of biological assays, mutation data, and structure activity relationships. (Doctoral Dissertation). University of North Carolina – Greensboro. Retrieved from http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=21355

Chicago Manual of Style (16^th Edition):

Lingerfelt, Mary A. “Construction and validation of GPR55 active and inactive state in silico models through the use of biological assays, mutation data, and structure activity relationships.” 2016. Doctoral Dissertation, University of North Carolina – Greensboro. Accessed March 02, 2021. http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=21355.

MLA Handbook (7^th Edition):

Lingerfelt, Mary A. “Construction and validation of GPR55 active and inactive state in silico models through the use of biological assays, mutation data, and structure activity relationships.” 2016. Web. 02 Mar 2021.

Vancouver:

Lingerfelt MA. Construction and validation of GPR55 active and inactive state in silico models through the use of biological assays, mutation data, and structure activity relationships. [Internet] [Doctoral dissertation]. University of North Carolina – Greensboro; 2016. [cited 2021 Mar 02]. Available from: http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=21355.

Council of Science Editors:

Lingerfelt MA. Construction and validation of GPR55 active and inactive state in silico models through the use of biological assays, mutation data, and structure activity relationships. [Doctoral Dissertation]. University of North Carolina – Greensboro; 2016. Available from: http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=21355

9. NC DOCKS at The University of North Carolina at Greensboro; Singh, Jagjeet. A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein.

Degree: 2014, NC Docks

URL: http://libres.uncg.edu/ir/uncg/f/Singh_uncg_0154D_11501.pdf

► One key signaling pathway in the cellular signaling involving G protein coupled receptors (GPCR) is via heterotrimeric G proteins. The first step in GPCR/G protein… (more)

▼ One key signaling pathway in the cellular signaling involving G protein coupled receptors (GPCR) is via heterotrimeric G proteins. The first step in GPCR/G protein signaling is the activation of a GPCR by the ligand binding and the next step is the activation of the G protein. Understanding the molecular mechanism behind the GPCR/G protein interactions will help in characterizing this important signaling pathway and should ultimately lead to the design of functionally selective ligands for this larger class of receptors. Earlier, the Reggio group used molecular dynamics simulations to study the activation of the cannabinoid CB2 receptor, a class A GPCR, by its endogenous ligand, 2-arachidonoylglycerol (2-AG) via the lipid bilayer. The goal of the current project was to study the next step in the G-protein mediated signal transduction, when an agonist activated CB2 receptor forms a complex with Gi protein and catalyzes the activation of Gi protein, releasing the guanosine diphosphate (GDP) bound between the ras-like (also known as GTPase domain) and helical domains of the Gá protein. To this end, we report here the CB2 / Gái1â1ã2 complex formation using our 2-AG activated CB2 receptor model. For G protein activation (dissociation of GDP), we hypothesized that GDP release from the ras-like and helical domains of Gái would be triggered by the hydration of GDP. We probed the role of the CB2 receptor interactions with the Gái protein and the resultant progression of GDP hydration. We have seen the number of waters surrounding GDP increase from 16 (t= 0 ns) to 28 waters (t=5 ìs). Two important interactions between the receptor and G-protein appear to lead to the increased hydration of GDP. (1) A hydrophobic interaction occurred between CB2 IC2 loop residue P139 and the Gái hydrophobic pocket residues: V34 (N terminus; L194 (â1 sheet); F196 (â2 sheet); and, F336, T340, I343, I344 (á5 helix) multiple times in our 5 ìs long trajectory. Each time this interaction occurred, an increase in GDP hydration was observed in our simulation. 2) We also observed an IC3 loop interaction with the Gái á4 helix between 1.4 to 1.6 ìs, in which the IC3 loop residue R229 reached to interact with E297 and E298. Taken together, our results show that the intracellular loops play a critical role in the hydration of GDP that should lead to G protein activation.

Subjects/Keywords: G proteins $x Receptors; Cannabinoids $x Receptors

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APA (6^th Edition):

NC DOCKS at The University of North Carolina at Greensboro; Singh, J. (2014). A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein. (Thesis). NC Docks. Retrieved from http://libres.uncg.edu/ir/uncg/f/Singh_uncg_0154D_11501.pdf

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

NC DOCKS at The University of North Carolina at Greensboro; Singh, Jagjeet. “A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein.” 2014. Thesis, NC Docks. Accessed March 02, 2021. http://libres.uncg.edu/ir/uncg/f/Singh_uncg_0154D_11501.pdf.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

NC DOCKS at The University of North Carolina at Greensboro; Singh, Jagjeet. “A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein.” 2014. Web. 02 Mar 2021.

Vancouver:

NC DOCKS at The University of North Carolina at Greensboro; Singh J. A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein. [Internet] [Thesis]. NC Docks; 2014. [cited 2021 Mar 02]. Available from: http://libres.uncg.edu/ir/uncg/f/Singh_uncg_0154D_11501.pdf.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

NC DOCKS at The University of North Carolina at Greensboro; Singh J. A model system for understanding cellular signaling of the cannabinoid CB2 receptor via the inhibitory Gi protein. [Thesis]. NC Docks; 2014. Available from: http://libres.uncg.edu/ir/uncg/f/Singh_uncg_0154D_11501.pdf

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Oregon State University

10. Venkataraman, Anand. In vitro and in vivo approaches for the functional characterization of the scaffold protein, GRASP.

Degree: PhD, Molecular and Cellular Biology, 2009, Oregon State University

URL: http://hdl.handle.net/1957/13654

► Studies using the pluripotent embryonic carcinoma cell line, P19, as a retinoic acid (RA)-responsive model system have been instrumental towards our understanding of the RA-dependent… (more)

▼ Studies using the pluripotent embryonic carcinoma cell line, P19, as a retinoic acid (RA)-responsive model system have been instrumental towards our understanding of the RA-dependent signaling pathways in development and homeostasis. Grp1-associated scaffold protein (GRASP; also known as Tamalin) was first identified by our group, as a gene robustly induced by RA treatment in P19 cells. GRASP was reported to influence the cell-surface expression of interacting membrane receptors in vitro albeit by an unknown mechanism. Furthermore, the in vivo role of GRASP is poorly understood. Mice with a germline deletion of Grasp (GRASP-/-) do not exhibit any gross morphological, behavioral or sexual deficits and exhibit mild, altered sensitivities to morphine and cocaine administration. The goals of our studies herein were to investigate the mechanistic details of GRASP for the role in trafficking and cell-surface, localization of membrane receptors in vitro and the role of GRASP in vivo. Previously, our group had identified a strong interaction of GRASP with Grp1, a guanine nucleotide exchange factor for the small G protein, Arf6. In this study we show GRASP localizes in intracellular recycling endosomal compartment(s), recruits Grp1 to these structures, and facilitates activation of Arf6. Activation of Arf6 regulates key aspects of vesicular trafficking, actin reorganization and cellular migration. Furthermore, we show that GRASP preferentially regulates intracellular membrane trafficking by the Arf6-dependent/clathrin-independent pathway. We have shown that GRASP is expressed in the adult murine skin. Our studies demonstrate a robust induction of GRASP transcripts in murine dermis and epidermis following exposure to ultraviolet (UV) rays. We also report the generation of novel mice with germline deletion of Grasp (GRASP-/-), that exhibit altered proliferative and apoptotic responses to UV exposure. Ongoing investigations suggest that the observed phenotypes of GRASP-/- mice after UV exposure maybe due to the dysregulation of the subcellular localization of the tumor suppressor protein, p53. Taken together, our in vitro and in vivo approaches have provided new insight in the role of GRASP as scaffold protein that regulates intracellular trafficking pathways. Advisors/Committee Members: Leid, Mark (advisor), Kioussi, Chrissa (committee member).

Subjects/Keywords: Trafficking; Cell receptors

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APA (6^th Edition):

Venkataraman, A. (2009). In vitro and in vivo approaches for the functional characterization of the scaffold protein, GRASP. (Doctoral Dissertation). Oregon State University. Retrieved from http://hdl.handle.net/1957/13654

Chicago Manual of Style (16^th Edition):

Venkataraman, Anand. “In vitro and in vivo approaches for the functional characterization of the scaffold protein, GRASP.” 2009. Doctoral Dissertation, Oregon State University. Accessed March 02, 2021. http://hdl.handle.net/1957/13654.

MLA Handbook (7^th Edition):

Venkataraman, Anand. “In vitro and in vivo approaches for the functional characterization of the scaffold protein, GRASP.” 2009. Web. 02 Mar 2021.

Vancouver:

Venkataraman A. In vitro and in vivo approaches for the functional characterization of the scaffold protein, GRASP. [Internet] [Doctoral dissertation]. Oregon State University; 2009. [cited 2021 Mar 02]. Available from: http://hdl.handle.net/1957/13654.

Council of Science Editors:

Venkataraman A. In vitro and in vivo approaches for the functional characterization of the scaffold protein, GRASP. [Doctoral Dissertation]. Oregon State University; 2009. Available from: http://hdl.handle.net/1957/13654

University of Utah

11. Roalstad, Shelly M. Receptor dynamics in virtual screening: A dihydrofolate reductase case study.

Degree: MS;, Pharmaceutics & Pharmaceutical Chemistry;, 2007, University of Utah

URL: http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/1634/rec/956

► The implications of receptor dynamics virtual screening were explored as part of proof of concept study for an interactive docking, molecular dynamics and scoring strategy.… (more)

▼ The implications of receptor dynamics virtual screening were explored as part of proof of concept study for an interactive docking, molecular dynamics and scoring strategy. The original study was to demonstrate whether or not the iterative process proposed would relax receptor structures that began as apo (without drug) or homology models toward known holo (with drug) coordinates. Due to species differences in the original receptor test systems, the study was refined to a set of well characterized dihydrofolate reductase (DHFR) receptors. Since both apo and holo structures were not available for each DHFR receptor selected, the goal of relaxing an apo structure toward a holo structure was modified. Various complexes of enzymes, ligand and cofactor were constructed to represent intermediates in the catalytic cycle know to adopt distinct conformations, and the new goal was to demonstrate movement toward one of these conformations during molecular dynamics simulations. Additionally, drug resistant E. coli DHFR and human DHFR structures were selected to probe the possible flexibility differences giving rise to enzymatic activity. Traditional molecular dynamics simulations demonstrated correct conformational change for one enzyme cofactor complex after 70 nanoseconds of simulation. Overall, relatively few complexes experienced any conformational change, indicating the need for longer trajectories or more advanced simulation techniques. Flexible regions of the enzyme described in literature were correctly depicted by trajectory analysis. Flexibility differences between bacterial and vertebrate DHFR showed bacterial DHFR to have more localized movements of three flexible loops and vertebrate DHFR more disperse flexibility. Evaluating the free energy of binding by Molecular Mechanics – Poisson Boltzmann Surface Area (MM-PBSA) methods was shown to be more insightful when employed before and after conformational change rather than over an entire trajectory. Ligand binding values generally independent of enzyme activity demonstrated the necessity of considering binding in the context of the catalytic cycle. Traditional molecular dynamics demonstrated the capability of moving a receptor toward a known conformation, through the resolution of conformational change was depended on the amount of trajectory available. Advanced molecular dynamics methods possible capable of expediting conformational change are proposed for future studies.

Subjects/Keywords: Drug Receptors; Drugs:

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APA (6^th Edition):

Roalstad, S. M. (2007). Receptor dynamics in virtual screening: A dihydrofolate reductase case study. (Masters Thesis). University of Utah. Retrieved from http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/1634/rec/956

Chicago Manual of Style (16^th Edition):

Roalstad, Shelly M. “Receptor dynamics in virtual screening: A dihydrofolate reductase case study.” 2007. Masters Thesis, University of Utah. Accessed March 02, 2021. http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/1634/rec/956.

MLA Handbook (7^th Edition):

Roalstad, Shelly M. “Receptor dynamics in virtual screening: A dihydrofolate reductase case study.” 2007. Web. 02 Mar 2021.

Vancouver:

Roalstad SM. Receptor dynamics in virtual screening: A dihydrofolate reductase case study. [Internet] [Masters thesis]. University of Utah; 2007. [cited 2021 Mar 02]. Available from: http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/1634/rec/956.

Council of Science Editors:

Roalstad SM. Receptor dynamics in virtual screening: A dihydrofolate reductase case study. [Masters Thesis]. University of Utah; 2007. Available from: http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/1634/rec/956

University of Utah

12. Osborne, Amber Valeria. The Modulatory Role of Neuronal Nicotinic Receptors on Peripheral Inflammation.

Degree: PhD, Pathology;, 2010, University of Utah

URL: http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/1089/rec/1195

► This dissertation examines the relationship between inflammatory cytokines and nicotinic acetylcholine receptors (nAChR). WT and nAChRa7 null mice were exposed to 4.8kJ/m2 of UVB on… (more)

▼ This dissertation examines the relationship between inflammatory cytokines and nicotinic acetylcholine receptors (nAChR). WT and nAChRa7 null mice were exposed to 4.8kJ/m2 of UVB on a standardized area of back skin. This dose of UVB caused the skin to be visibly inflamed 48 hours after exposure; at this point the back skin was removed and analyzed for inflammatory cytokines. Production of IL-lp and IL-6, but not TNFa was significantly increased in a 7 null mice. Further, H&E stained skin sections revealed greater edema in mice lacking a7. Production of SOCS3, a negative regulator of cytokines, was decreased in inflamed skin from a7 null mice, suggesting a potential mechanism by which a7 could regulate cytokine production. The induction of IL-1(3 and IL-6 in skin by UVB was inhibited in mice first exposed to y-irradiation, suggesting that rapidly dividing cells that infiltrate the inflamed skin were responsible for the measured cytokine production. To further identify the types of cells infiltrating the skin following an inflammatory stimulus, croton oil was applied to mouse ears and infiltrating cells were isolated following the separation of dorsal and ventral ear flaps. Mice lacking a7 had a significant increase in the total number of recruited cells as well as increased expression of IL-lp, IL-6 and TNFa by infiltrating cells. The cells infiltrating the inflamed site were determined to be CD1 lb+ Ly6g+ neutrophils and CD1 lb+ F4/80+ macrophages by FACS analysis. Further, it was determined that chemokines which recruit neutrophils and macrophages, such as CXCL2, CXCL5 and CCL3 were all also increased in a7 null mice. Inhibiting the p38 MAP Kinase signaling pathway in WT and a 7 null primary macrophage cultures decreased the LPS induced expression of cytokines and chemokines. The reciprocal effect of cytokines on nicotinic receptors was also investigated. It was determined that treatment of transfected HEK293 cells with TNFa induces enhanced upregulation of the high affinity nicotine binding receptor a4p2. Treatment of these cells with a p38 MAP Kinase inhibitor blocks the TNFa enhanced upregulation. Collectively, these data demonstrate a relationship between nicotinic receptors and inflammatory cytokines and the involvement of the p38 MAP Kinase pathway.

Subjects/Keywords: Nicotine Receptors; Inflammation

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APA (6^th Edition):

Osborne, A. V. (2010). The Modulatory Role of Neuronal Nicotinic Receptors on Peripheral Inflammation. (Doctoral Dissertation). University of Utah. Retrieved from http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/1089/rec/1195

Chicago Manual of Style (16^th Edition):

Osborne, Amber Valeria. “The Modulatory Role of Neuronal Nicotinic Receptors on Peripheral Inflammation.” 2010. Doctoral Dissertation, University of Utah. Accessed March 02, 2021. http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/1089/rec/1195.

MLA Handbook (7^th Edition):

Osborne, Amber Valeria. “The Modulatory Role of Neuronal Nicotinic Receptors on Peripheral Inflammation.” 2010. Web. 02 Mar 2021.

Vancouver:

Osborne AV. The Modulatory Role of Neuronal Nicotinic Receptors on Peripheral Inflammation. [Internet] [Doctoral dissertation]. University of Utah; 2010. [cited 2021 Mar 02]. Available from: http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/1089/rec/1195.

Council of Science Editors:

Osborne AV. The Modulatory Role of Neuronal Nicotinic Receptors on Peripheral Inflammation. [Doctoral Dissertation]. University of Utah; 2010. Available from: http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/1089/rec/1195

13. Visic, Petra. The role of the Sigma1 receptor (σ1R) in store-operated calcium entry (SOCE) microdomains.

Degree: PhD, 2020, University of Sussex

URL: http://sro.sussex.ac.uk/id/eprint/90959/ ; https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.804978

► The Sigma1 receptor (σ1R) is an endoplasmic reticulum (ER) chaperone targeted to mitochondrion associated ER membranes (MAMs). The upregulation of σ1R is associated with various… (more)

▼ The Sigma1 receptor (σ1R) is an endoplasmic reticulum (ER) chaperone targeted to mitochondrion associated ER membranes (MAMs). The upregulation of σ1R is associated with various cancers, whereas the decreased expression and mutant forms of σ1R are associated with neurodegenerative disorders. The underlying cellular mechanism by which σ1R exerts such a versatile impact remains elusive. At MAMs, σ1R is reported to regulate inter-organelle Ca2+ levels. Following translocation to ER-plasma membrane junctions, σ1R is reported to interact with various ion channels, including the key regulators of store-operated Ca2+ entry (SOCE). I have investigated the role of σ1R in the regulation of SOCE within a population of cells and within the SOCE microdomains of single cells. In a population of cells, overexpression of σ1R profoundly inhibited both Ca2+ store content and SOCE. Although these measurements of global [Ca2+]cyt provide essential information about the functional role of σ1R in the regulation of SOCE, they do not provide detailed information about the effects of σ1R on temporal and spatial aspects of SOCE within the microdomain of the ER-plasma membrane junction. Recently developed, the G-GECO1.2-Orai1 construct encodes for a fully functional Orai1 protein with a genetically encoded fluorescent Ca2+ reporter protein. The Orai1 channel is a key regulator of SOCE. GECO1.2-Orai1 allows for the monitoring of Orai1 channel activity in SOCE microdomains. Within the SOCE microdomains, overexpression of σ1R reduced the frequency of highly-activated G-GECO1.2-Orai1 clusters, which resulted in cumulatively low SOCE. Overexpression of σ1RE102Q, an ALS-causing mutant, failed to inhibit SOCE. In situ, σ1R was shown to interact with another key regulator of SOCE, STIM1 and its less-studied homolog STIM2. Overexpression of σ1R resulted in the inhibition of STIM2.2-mediated SOCE triggered by the ER Ca2+ store depletion. σ1R failed to inhibit STIM2.2-mediated SOCE during basal conditions, suggesting that regulation of SOCE by σ1R requires a greater drop in ER [Ca2+] than occurs under basal conditions.

Subjects/Keywords: RM0301.41 Drug receptors

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APA (6^th Edition):

Visic, P. (2020). The role of the Sigma1 receptor (σ1R) in store-operated calcium entry (SOCE) microdomains. (Doctoral Dissertation). University of Sussex. Retrieved from http://sro.sussex.ac.uk/id/eprint/90959/ ; https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.804978

Chicago Manual of Style (16^th Edition):

Visic, Petra. “The role of the Sigma1 receptor (σ1R) in store-operated calcium entry (SOCE) microdomains.” 2020. Doctoral Dissertation, University of Sussex. Accessed March 02, 2021. http://sro.sussex.ac.uk/id/eprint/90959/ ; https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.804978.

MLA Handbook (7^th Edition):

Visic, Petra. “The role of the Sigma1 receptor (σ1R) in store-operated calcium entry (SOCE) microdomains.” 2020. Web. 02 Mar 2021.

Vancouver:

Visic P. The role of the Sigma1 receptor (σ1R) in store-operated calcium entry (SOCE) microdomains. [Internet] [Doctoral dissertation]. University of Sussex; 2020. [cited 2021 Mar 02]. Available from: http://sro.sussex.ac.uk/id/eprint/90959/ ; https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.804978.

Council of Science Editors:

Visic P. The role of the Sigma1 receptor (σ1R) in store-operated calcium entry (SOCE) microdomains. [Doctoral Dissertation]. University of Sussex; 2020. Available from: http://sro.sussex.ac.uk/id/eprint/90959/ ; https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.804978

Nelson Mandela Metropolitan University

14. Van Zyl, Dwain George. Production of recombinant human CD21 and CD23 : towards a better understanding of their interaction.

Degree: MSc, Faculty of Science, 2013, Nelson Mandela Metropolitan University

URL: http://hdl.handle.net/10948/d10211135

► The prevalence of allergic diseases has dramatically increased over the last three decades. Presently, it is estimated that 20-30 per cent of the developed world… (more)

▼ The prevalence of allergic diseases has dramatically increased over the last three decades. Presently, it is estimated that 20-30 per cent of the developed world suffers from allergic diseases. The majority of allergic diseases are rooted in the activities of IgE; an immunoglobulin which exerts its effector functions by interacting with a network of proteins. This network includes its low affinity receptor CD23. Cross linking of membrane IgE and CD21 by soluble CD23 results in an increase in IgE synthesis. This marks the interaction between CD23 and CD21 as an attractive therapeutic target. However, details regarding this interaction are inadequate for rational drug design. To obtain a deeper understanding of the CD23-CD21 interaction recombinant human CD21 (SCR1-2 and SCR5-8) and CD23 (16 kD and 25 kDa) were produced. The cloning, expression and purification of recombinant proteins comprised a significant portion of this study. Recombinant CD23 was expressed as inclusion bodies, refolded by rapid dilution and purified by size exclusion chromatography. Conversely, recombinant CD21 was expressed as soluble MBP-fusions and purified with an amylose affinity resin. The interaction between recombinant CD23 and CD21 was analysed by flow cytometry and ELISA experiments. Flow cytometry showed that 16 kDa and 25 kDa CD23 interacted with SCR5-8 to the same extent. Semi-quantitative ELISA experiments showed that both SCR1-2 and SCR5-8 were able to interact with 16 kDa and 25 kDa CD23. This suggests that the binding sites of SCR1-2 and SCR5-8 occur on 16 kDa CD23. Furthermore, since proteins were expressed in E. coli it suggests that the CD23-CD21 interaction does not require glycosylation. Furthermore, considering what is known about the SCR1-2-CD23 interaction from previous NMR studies; i.e. that the C-terminal tail (residues residues 289-298) of CD23 is responsible for binding SCR1-2, indicates that SCR5-8 binds somewhere within the lectin domain of CD23. This indicates that the CD23-CD21 interaction involves C-terminal tail-SCR1-2 and lectin domain-SCR5-8 interactions. Advisors/Committee Members: Oosthuizen, V Dr.

Subjects/Keywords: Immunoglobulins; Fc receptors

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APA (6^th Edition):

Van Zyl, D. G. (2013). Production of recombinant human CD21 and CD23 : towards a better understanding of their interaction. (Masters Thesis). Nelson Mandela Metropolitan University. Retrieved from http://hdl.handle.net/10948/d10211135

Chicago Manual of Style (16^th Edition):

Van Zyl, Dwain George. “Production of recombinant human CD21 and CD23 : towards a better understanding of their interaction.” 2013. Masters Thesis, Nelson Mandela Metropolitan University. Accessed March 02, 2021. http://hdl.handle.net/10948/d10211135.

MLA Handbook (7^th Edition):

Van Zyl, Dwain George. “Production of recombinant human CD21 and CD23 : towards a better understanding of their interaction.” 2013. Web. 02 Mar 2021.

Vancouver:

Van Zyl DG. Production of recombinant human CD21 and CD23 : towards a better understanding of their interaction. [Internet] [Masters thesis]. Nelson Mandela Metropolitan University; 2013. [cited 2021 Mar 02]. Available from: http://hdl.handle.net/10948/d10211135.

Council of Science Editors:

Van Zyl DG. Production of recombinant human CD21 and CD23 : towards a better understanding of their interaction. [Masters Thesis]. Nelson Mandela Metropolitan University; 2013. Available from: http://hdl.handle.net/10948/d10211135

Texas Tech University

15. Lokubandara, Anuththara Hemamali. Computational and functional analysis of human bitter taste receptors.

Degree: MS, Biotechnology, 2018, Texas Tech University

URL: http://hdl.handle.net/2346/73804

► Mammals perceive five tastes: sweet, umami, salty, sour, and bitter. The focus of this study is related to the sense of taste or gustation. The… (more)

▼ Mammals perceive five tastes: sweet, umami, salty, sour, and bitter. The focus of this study is related to the sense of taste or gustation. The sense of taste enables an animal to discriminate nourishment from toxins. The sense of taste is mediated by taste receptor cells. These cells are localized and organized within taste buds. Taste receptor cells are primarily found within the oral cavity, typically on the dorsal surface of the tongue, palate, the oropharynx. There are two taste receptor protein families in mammals: T1R and T2R. Taste receptors are members of the G-protein coupled receptor super family (GPCR). Sequence homology assessments of these receptors place them in two categories: the T1R family is classified as class C; whereas, T2Rs are categorized as class A GPCRs. Twenty-Five T2Rs or bitter taste receptors have been identified in humans. Bitter taste receptors are characterized by seven transmembrane domains along with short amino and carboxyl termini-Class A GPCRs. Most of the research carried out thus far has focused on sweet and umami taste receptors. Bitter taste receptor studies have focused on receptors with known ligands that can activate them. The objective of this study is to elucidate the mechanism of the interactions between bitter taste receptors and tastants (or compounds that elicit a response from a bitter taste receptor). We utilized high-throughput and computationally-derived processes have been utilized to build models for a rational set of receptors; subsequently, we docked the experimentally known agonists with each receptor. Two strategies were adopted for docking-targeted and automatic. Theoretically, approximately, nine hundred receptor-ligand interactions in this high throughput endeavor were assessed. Realistically however, five hundred and seventy-nine interactions were feasible and available for further analysis. Automated docking was not only observed to be always energetically favorable, but also a high number of conformations were observed when compared to targeted docking. Specific residues were identified associated with many ligands for a specific receptor. Common residues were observed to be associated with similar functional groups of ligands. Advisors/Committee Members: Tripathy, Jatindra N (committee member), San-Francisco, Susan (committee member), Crasto, Chiquito J. (Committee Chair).

Subjects/Keywords: Bitter Taste Receptors

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APA (6^th Edition):

Lokubandara, A. H. (2018). Computational and functional analysis of human bitter taste receptors. (Masters Thesis). Texas Tech University. Retrieved from http://hdl.handle.net/2346/73804

Chicago Manual of Style (16^th Edition):

Lokubandara, Anuththara Hemamali. “Computational and functional analysis of human bitter taste receptors.” 2018. Masters Thesis, Texas Tech University. Accessed March 02, 2021. http://hdl.handle.net/2346/73804.

MLA Handbook (7^th Edition):

Lokubandara, Anuththara Hemamali. “Computational and functional analysis of human bitter taste receptors.” 2018. Web. 02 Mar 2021.

Vancouver:

Lokubandara AH. Computational and functional analysis of human bitter taste receptors. [Internet] [Masters thesis]. Texas Tech University; 2018. [cited 2021 Mar 02]. Available from: http://hdl.handle.net/2346/73804.

Council of Science Editors:

Lokubandara AH. Computational and functional analysis of human bitter taste receptors. [Masters Thesis]. Texas Tech University; 2018. Available from: http://hdl.handle.net/2346/73804

16. Chew, Geoffrey H. Manipulation of α-Bungarotoxin Binding Sites in Nicotinic Acetylcholine Receptors to Elucidate Fundamental Aspects of Receptor Function.

Degree: PhD, Molecular Pharmacology, Physiology, and Biotechnology, 2011, Brown University

URL: https://repository.library.brown.edu/studio/item/bdr:11163/

► Nicotinic acetylcholine receptors (nAChRs) mediate excitatory neurotransmission at synapses throughout the body in the neuromuscular junction and the central nervous system. The two basic types… (more)

Subjects/Keywords: nicotinic acetylcholine receptors

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APA (6^th Edition):

Chew, G. H. (2011). Manipulation of α-Bungarotoxin Binding Sites in Nicotinic Acetylcholine Receptors to Elucidate Fundamental Aspects of Receptor Function. (Doctoral Dissertation). Brown University. Retrieved from https://repository.library.brown.edu/studio/item/bdr:11163/

Chicago Manual of Style (16^th Edition):

Chew, Geoffrey H. “Manipulation of α-Bungarotoxin Binding Sites in Nicotinic Acetylcholine Receptors to Elucidate Fundamental Aspects of Receptor Function.” 2011. Doctoral Dissertation, Brown University. Accessed March 02, 2021. https://repository.library.brown.edu/studio/item/bdr:11163/.

MLA Handbook (7^th Edition):

Chew, Geoffrey H. “Manipulation of α-Bungarotoxin Binding Sites in Nicotinic Acetylcholine Receptors to Elucidate Fundamental Aspects of Receptor Function.” 2011. Web. 02 Mar 2021.

Vancouver:

Chew GH. Manipulation of α-Bungarotoxin Binding Sites in Nicotinic Acetylcholine Receptors to Elucidate Fundamental Aspects of Receptor Function. [Internet] [Doctoral dissertation]. Brown University; 2011. [cited 2021 Mar 02]. Available from: https://repository.library.brown.edu/studio/item/bdr:11163/.

Council of Science Editors:

Chew GH. Manipulation of α-Bungarotoxin Binding Sites in Nicotinic Acetylcholine Receptors to Elucidate Fundamental Aspects of Receptor Function. [Doctoral Dissertation]. Brown University; 2011. Available from: https://repository.library.brown.edu/studio/item/bdr:11163/

Hong Kong University of Science and Technology

17. Ren, Lihuan. GABA_A receptor subtype selectivity and structure-activity relationships of flavonoids.

Degree: 2011, Hong Kong University of Science and Technology

URL: http://repository.ust.hk/ir/Record/1783.1-7346 ; https://doi.org/10.14711/thesis-b1155315 ; http://repository.ust.hk/ir/bitstream/1783.1-7346/1/th_redirect.html

► A flavonoid, 6-hydroxyflavone, was previously reported to bind to the benzodiazepine (BZ) site on GABA_A receptors with moderate binding affinity. In the present study, we… (more)

▼ A flavonoid, 6-hydroxyflavone, was previously reported to bind to the benzodiazepine (BZ) site on GABA_A receptors with moderate binding affinity. In the present study, we showed that 6-hydroxyflavone partially potentiated GABA-induced currents in native GABA_A receptors expressed in cortical neurons via BZ site, as the enhancement was blocked by the antagonist flumazenil. Furthermore, in patch clamp studies, 6-hydroxyflavone displayed significant preference for α2- and α3-containing subtypes, which were thought to mediate anxiolytic effect, compared to α1- and α5-containing subtypes expressed in HEK 293T cells. In mice, 6-hydroxyflavone exhibited anxiolytic-like effect in the elevated plus-maze test, unaccompanied by the sedative, cognitive impairing, myorelaxant, motor incoordination and anticonvulsant effects when tested in the hole-board, step-through passive avoidance, horizontal wire, rotarod, and pentylenetetrazol (PTZ)-induced seizure tests, respectively. The findings therefore identified 6-hydroxyflavone as a promising drug candidate for the treatment of anxiety-like disorders. In addition, GABA_A receptor structure-efficacy relationships for flavones were also studied. The present study focused on flavone 6-substitution, implied in previous studies being relevant to efficacy. Structure analogues, each varying only at position 6, were compared, including 6-fluoroflavone, 6-chloroflavone, 6-bromoflavone, and 2’-hydroxyflavone analyzed in the present study, as well as 6,2’-dihydroxyflavone reported earlier. Whole-cell patch clamp and animal behavior experiments demonstrated 6-bromoflavone to be a positive modulator at GABA_A receptors acting through benzodiazepine site. In contrast, the other two 6-haloflavones were both neutralizing modulators. Moreover, 2’-hydroxyflavone was shown to be a neutralizing modulator, different in efficacy from its structural analogue, 6,2’-dihydroxyflavone, a negative modulator of GABA_A receptors. The fact that flavone analogues differing only at position 6 showed drastically different pharmacological properties clearly points to 6-substitution being an important determinant of efficacy. The results suggest that a large width of the first atom on the 6-substituent favors a high binding affinity of the 6-substituted flavone, whereas a large overall volume of the 6-substituent favors positive modulator activity, which could be modified by, e.g., 2’-hydroxyl substitution. These findings have contributed to the understanding of quantitative structure-efficacy relationships for flavones acting at GABA_A receptors, and hence facilitation of flavone-based drug development.

Subjects/Keywords: GABA – Receptors ; Flavonoids

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Ren, L. (2011). GABA_A receptor subtype selectivity and structure-activity relationships of flavonoids. (Thesis). Hong Kong University of Science and Technology. Retrieved from http://repository.ust.hk/ir/Record/1783.1-7346 ; https://doi.org/10.14711/thesis-b1155315 ; http://repository.ust.hk/ir/bitstream/1783.1-7346/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Ren, Lihuan. “GABA_A receptor subtype selectivity and structure-activity relationships of flavonoids.” 2011. Thesis, Hong Kong University of Science and Technology. Accessed March 02, 2021. http://repository.ust.hk/ir/Record/1783.1-7346 ; https://doi.org/10.14711/thesis-b1155315 ; http://repository.ust.hk/ir/bitstream/1783.1-7346/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Ren, Lihuan. “GABA_A receptor subtype selectivity and structure-activity relationships of flavonoids.” 2011. Web. 02 Mar 2021.

Vancouver:

Ren L. GABA_A receptor subtype selectivity and structure-activity relationships of flavonoids. [Internet] [Thesis]. Hong Kong University of Science and Technology; 2011. [cited 2021 Mar 02]. Available from: http://repository.ust.hk/ir/Record/1783.1-7346 ; https://doi.org/10.14711/thesis-b1155315 ; http://repository.ust.hk/ir/bitstream/1783.1-7346/1/th_redirect.html.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Ren L. GABA_A receptor subtype selectivity and structure-activity relationships of flavonoids. [Thesis]. Hong Kong University of Science and Technology; 2011. Available from: http://repository.ust.hk/ir/Record/1783.1-7346 ; https://doi.org/10.14711/thesis-b1155315 ; http://repository.ust.hk/ir/bitstream/1783.1-7346/1/th_redirect.html

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

University of North Carolina – Greensboro

18. Pyle, Jennifer L. Identification of agonist and antagonist binding sites at the G-Protein Coupled Receptor, GPR18.

Degree: 2015, University of North Carolina – Greensboro

URL: http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=19120

► GPR18, a member of the Class A G-Protein Coupled Receptors (GPCRs), is recently a de-orphanized receptor, that upon activation has been found to boost the… (more)

▼ GPR18, a member of the Class A G-Protein Coupled Receptors (GPCRs), is recently a de-orphanized receptor, that upon activation has been found to boost the immune system. Although a GPR18 crystal structure has not been solved, a homology model of the inactive state (R) of GPR18 was built in the Reggio lab based upon the mu-opioid x-ray crystal structure. The present study continues this work by adding loop regions and N- and C-termini to the R state model and by developing a model of GPR18 R* (Active) state, complete with loop regions and N- and C-termini. The complete inactive and active state models were used for docking studies of five known GPR18 antagonists, 1,3-dimethoxy-5-methyl-2-[(1R,6R)-3-methyl-6-prop-1-en-2-ylcyclohex-2-en-1-yl]benzene; 1, (Z)-2-(3((4-chlorobenzyl)oxy)benzylidene)-3-methylene-2,3,6,7-tetrahydro-5H-imidazo[2,1-b][1,3]thiazine; 2, (1R,2R)-2',6'-dimethoxy-4',5-dimethyl-2-(prop-1-en-2-yl)-1,2,3,4-tetrahydro-1,1'-biphenyl; 3, (Z)-2-(3-(4-chlorobenzyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1-b][1,3]thiazin-3(5H)-one; 4, and 2-[(1R,6R)-6-isopropenyl-3-methylcyclohex-2-en-1-yl]-5-pentylbenzene-1,3-diol; 5 and the GPR18 endogenous ligand, N-arachidonylglycine (NAGly). Conformational searches were performed on all antagonists using a systematic search using the Hartree-Fock method at the 6-31G* level of theory. Because NAGly is highly flexible, its low energy conformations were determined using the Conformational Memories method. All low energy conformations, less than 3.0 kcal/mol, of each ligand were docked using Glide into their respective bundles based on the state of the receptor each ligand stabilizes. The key interaction site for all antagonists, an ARG in TMH5, R5.42, anchors each antagonist in the TMH bundle such that rotameric changes in key toggle switch residues, F6.48/H6.52, are prevented, thus preventing the activation of the receptor. The extracellular loop 2 (EC2 loop) residue Y160 further stabilizes each antagonist in the binding site. Identified interactions result in Glide scores consistent with experimental EC50 data. The primary interaction site for the agonist, NAGly, was TMH2 residue R2.60. An additional NAGly interaction was identified with the EC2 loop residue K174. Mutation experiments of key residues identified here are underway in a collaborator’s lab. These studies will help confirm the importance of these key residues and further our understanding of the receptor.; Activation, Binding sites, GPCR, GPR18, Models, Receptor Advisors/Committee Members: Patricia Reggio (advisor).

Subjects/Keywords: G proteins – Receptors

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Pyle, J. L. (2015). Identification of agonist and antagonist binding sites at the G-Protein Coupled Receptor, GPR18. (Masters Thesis). University of North Carolina – Greensboro. Retrieved from http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=19120

Chicago Manual of Style (16^th Edition):

Pyle, Jennifer L. “Identification of agonist and antagonist binding sites at the G-Protein Coupled Receptor, GPR18.” 2015. Masters Thesis, University of North Carolina – Greensboro. Accessed March 02, 2021. http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=19120.

MLA Handbook (7^th Edition):

Pyle, Jennifer L. “Identification of agonist and antagonist binding sites at the G-Protein Coupled Receptor, GPR18.” 2015. Web. 02 Mar 2021.

Vancouver:

Pyle JL. Identification of agonist and antagonist binding sites at the G-Protein Coupled Receptor, GPR18. [Internet] [Masters thesis]. University of North Carolina – Greensboro; 2015. [cited 2021 Mar 02]. Available from: http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=19120.

Council of Science Editors:

Pyle JL. Identification of agonist and antagonist binding sites at the G-Protein Coupled Receptor, GPR18. [Masters Thesis]. University of North Carolina – Greensboro; 2015. Available from: http://libres.uncg.edu/ir/listing.aspx?styp=ti&id=19120

University of Aberdeen

19. Dorning, Ashley J. The pharmacology, signalling and expression of the lipid-sensing receptor GPR92.

Degree: PhD, 2013, University of Aberdeen

URL: https://abdn.alma.exlibrisgroup.com/view/delivery/44ABE_INST/12152684420005941 ; https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.582731

► G protein-coupled receptors (GPCRs) are 7 transmembrane domain proteins capable of initiating cellular responses following ligand binding. GPR92 is expressed in the central nervous system… (more)

▼ G protein-coupled receptors (GPCRs) are 7 transmembrane domain proteins capable of initiating cellular responses following ligand binding. GPR92 is expressed in the central nervous system (CNS) and is demonstrated to be involved in pain signalling via neurons of the spinal cord and dorsal root ganglion (DRG). Activated by the endogenous lipid lysophosphatidic acid (LPA), GPR92 is now considered the 5th LPA receptor. There remains controversy regarding GPR92 pharmacology however, as studies show another endogenous lipid, farnesyl pyrophosphate (FPP), also activates GPR92 with similar potency and efficacy to LPA. LPA-induced activation of GPR92 results in increased intracellular calcium (Ca2+) and cAMP. Furthermore, GPR92 mediates neurite retraction via Rho kinase and activates the cAMP responsive element-binding (CREB) protein. This transcription factor is important in synaptic plasticity and regulates the expression of many neuronal genes including brain derived neurotrophic factor (BDNF), yet the role of GPR92 in the brain has not been explored. Here, I describe the pharmacology and signalling of GPR92, with preliminary data describing its expression. I utilise a cell line lacking endogenous LPA responsiveness (B103 rat neuroblastoma) in which I stably express GPR92. Using intracellular Ca2+ changes and CREB phosphorylation as read-outs, I find FPP to be the most potent and efficacious ligand. The similarly structured lipid geranylgeranyl pyrophosphate (GGPP) produced comparable results to FPP. GPR92-mediated CREB phosphorylation has been described in a mouse model of pain. The ligands which induce this response however, have not been assessed. I describe for the first time, ligand-induced CREB phosphorylation via GPR92, and found that FPP causes the most robust CREB response. LPA and GGPP also induced GPR92-mediated CREB phsphorylation. Furthermore, I find that GPR92 mediates a novel Gq-dependent, Ca2+ independent, signalling pathway resulting in CREB phosphorylation. In addition, I examine GPR92 expression in the CNS using reverse-transcriptase polymerase chain reaction (RT-PCR) and in situ hybridisation. GPR92 is expressed throughout the brain, with particularly high expression in 7 the brain stem, DRG, and hippocampus. In situ hybridisation revealed a distinct expression pattern confirming high levels of GPR92 mRNA in the hippocampal region. GPR92 mRNA is also observed in the cortex, habenula, thalamus and hypothalamus. I also report the expression of the FPP synthesising enzyme FPP synthase (FPPS). Relative expression levels of FPPS between CNS regions are similar to GPR92. Preliminary data suggests FPP is capable of mobilising Ca2+ in hippocampal neuronal and non-neuronal cells. These data suggest an important role for GPR92 in the brain where it, and the enzyme involved in generating one of its endogenous ligands, are highly expressed.

Subjects/Keywords: 610; Cell receptors

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Dorning, A. J. (2013). The pharmacology, signalling and expression of the lipid-sensing receptor GPR92. (Doctoral Dissertation). University of Aberdeen. Retrieved from https://abdn.alma.exlibrisgroup.com/view/delivery/44ABE_INST/12152684420005941 ; https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.582731

Chicago Manual of Style (16^th Edition):

Dorning, Ashley J. “The pharmacology, signalling and expression of the lipid-sensing receptor GPR92.” 2013. Doctoral Dissertation, University of Aberdeen. Accessed March 02, 2021. https://abdn.alma.exlibrisgroup.com/view/delivery/44ABE_INST/12152684420005941 ; https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.582731.

MLA Handbook (7^th Edition):

Dorning, Ashley J. “The pharmacology, signalling and expression of the lipid-sensing receptor GPR92.” 2013. Web. 02 Mar 2021.

Vancouver:

Dorning AJ. The pharmacology, signalling and expression of the lipid-sensing receptor GPR92. [Internet] [Doctoral dissertation]. University of Aberdeen; 2013. [cited 2021 Mar 02]. Available from: https://abdn.alma.exlibrisgroup.com/view/delivery/44ABE_INST/12152684420005941 ; https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.582731.

Council of Science Editors:

Dorning AJ. The pharmacology, signalling and expression of the lipid-sensing receptor GPR92. [Doctoral Dissertation]. University of Aberdeen; 2013. Available from: https://abdn.alma.exlibrisgroup.com/view/delivery/44ABE_INST/12152684420005941 ; https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.582731

Rutgers University

20. Sanner, James William, 1987-. Identification and characterization of components of rab-6-mediated trafficking in caenorhabditus elegans.

Degree: MS, Microbiology and Molecular Genetics, 2014, Rutgers University

URL: https://rucore.libraries.rutgers.edu/rutgers-lib/45448/

► Membrane trafficking in neurons is an important mechanism used to regulate signaling. Controlling the abundance of AMPA-type receptors at the synapse is important for synaptic… (more)

▼ Membrane trafficking in neurons is an important mechanism used to regulate signaling. Controlling the abundance of AMPA-type receptors at the synapse is important for synaptic plasticity and influences processes involved in learning, memory formation, and motor control (Greger and Esteban, 2007; Shepherd and Huganir, 2007). In Caenorhabditis elegans, recycling of the AMPA receptor subunit GLR-1 has been demonstrated to be one method by which synaptic signaling mechanisms can be controlled. Rab GTPases 6.1 and 6.2 have been profiled for their role in trafficking of GLR-1 in neurons. RAB-6.2 plays a role in the retrograde trafficking of the AMPA-type glutamate receptor GLR-1 (Zhang et al., 2012). Activated Rab GTPases regulate membrane trafficking by recruiting multiple effectors, including proteins that modify phospholipid membrane composition, motor proteins that tether membranes to the cytoskeleton, and scaffolding proteins that bind to specific proteins within membranes (Stenmark, 2009). In order to understand RAB-6.2 function, we used a yeast two-hybrid approach to screen for candidate effector molecules. Herein, we discuss the screen performed and detail candidates of interest. We identified one particularly compelling candidate, a phosphoinositol-5-phosphatase named SAC-2, which we hypothesize to be involved in vesicle uncoating and/or in modifying membrane phospholipids. SAC-2::GFP is localized to punctate structures along the ventral nerve cord and in the neuron soma. SAC-2::GFP localization to puncta in the soma is enhanced in rab-6.2(ok2254) null mutant animals, which is opposite to our expectation for RAB-6.2 retrograde cargo or effector molecules. Additionally, we assessed the overlap in functions between RAB-6.1 and RAB-6.2, and delineating their pathways. In agreement with previous data from our lab, our findings suggest that the two RAB-6 isoforms perform similar trafficking functions, but do so independently of each other. Advisors/Committee Members: Padgett, Richard (chair), Firestein, Bonnie (internal member), Grant, Barth (internal member), Rongo, Christopher (internal member).

Subjects/Keywords: Glutamic acid – Receptors

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APA (6^th Edition):

Sanner, James William, 1. (2014). Identification and characterization of components of rab-6-mediated trafficking in caenorhabditus elegans. (Masters Thesis). Rutgers University. Retrieved from https://rucore.libraries.rutgers.edu/rutgers-lib/45448/

Chicago Manual of Style (16^th Edition):

Sanner, James William, 1987-. “Identification and characterization of components of rab-6-mediated trafficking in caenorhabditus elegans.” 2014. Masters Thesis, Rutgers University. Accessed March 02, 2021. https://rucore.libraries.rutgers.edu/rutgers-lib/45448/.

MLA Handbook (7^th Edition):

Sanner, James William, 1987-. “Identification and characterization of components of rab-6-mediated trafficking in caenorhabditus elegans.” 2014. Web. 02 Mar 2021.

Vancouver:

Sanner, James William 1. Identification and characterization of components of rab-6-mediated trafficking in caenorhabditus elegans. [Internet] [Masters thesis]. Rutgers University; 2014. [cited 2021 Mar 02]. Available from: https://rucore.libraries.rutgers.edu/rutgers-lib/45448/.

Council of Science Editors:

Sanner, James William 1. Identification and characterization of components of rab-6-mediated trafficking in caenorhabditus elegans. [Masters Thesis]. Rutgers University; 2014. Available from: https://rucore.libraries.rutgers.edu/rutgers-lib/45448/

Rutgers University

21. Sharp, Liam M., 1989-. Coarse-grained simulations of nicotinic acetylcholine receptors in complex mixed membranes: embedded lipids and domain partitioning.

Degree: MS, Computational and Integrative Biology, 2016, Rutgers University

URL: https://rucore.libraries.rutgers.edu/rutgers-lib/49832/

► Nicotinic acetylcholine receptors (nAChRs) are pentameric Ligand Gated Ion Channels that are critical to signaling across synapses and the neuromuscular junction; such signaling is facilitated… (more)

Subjects/Keywords: Lipids; Nicotinic receptors

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Sharp, Liam M., 1. (2016). Coarse-grained simulations of nicotinic acetylcholine receptors in complex mixed membranes: embedded lipids and domain partitioning. (Masters Thesis). Rutgers University. Retrieved from https://rucore.libraries.rutgers.edu/rutgers-lib/49832/

Chicago Manual of Style (16^th Edition):

Sharp, Liam M., 1989-. “Coarse-grained simulations of nicotinic acetylcholine receptors in complex mixed membranes: embedded lipids and domain partitioning.” 2016. Masters Thesis, Rutgers University. Accessed March 02, 2021. https://rucore.libraries.rutgers.edu/rutgers-lib/49832/.

MLA Handbook (7^th Edition):

Sharp, Liam M., 1989-. “Coarse-grained simulations of nicotinic acetylcholine receptors in complex mixed membranes: embedded lipids and domain partitioning.” 2016. Web. 02 Mar 2021.

Vancouver:

Sharp, Liam M. 1. Coarse-grained simulations of nicotinic acetylcholine receptors in complex mixed membranes: embedded lipids and domain partitioning. [Internet] [Masters thesis]. Rutgers University; 2016. [cited 2021 Mar 02]. Available from: https://rucore.libraries.rutgers.edu/rutgers-lib/49832/.

Council of Science Editors:

Sharp, Liam M. 1. Coarse-grained simulations of nicotinic acetylcholine receptors in complex mixed membranes: embedded lipids and domain partitioning. [Masters Thesis]. Rutgers University; 2016. Available from: https://rucore.libraries.rutgers.edu/rutgers-lib/49832/

22. Court Lecuyer, Nathalie. Intéractions hôte-pathogène : rôle des pattern recognition receptors (PRR) dans l'induction de la réponse immunitaire aux mycobactéries et modulation de cette réponse par des composés mycobactériens : Host-pathogen interactions : role of pattern recognition receptors (PRR) for the induction of the host immune response in response to mycobacteria and modulation of this response by mycobacterial components.

Degree: Docteur es, Biologie cellulaire et moléculaire. Immunologie, 2010, Université d'Orléans

URL: http://www.theses.fr/2010ORLE2087

►

Nos travaux ont permis d’étudier différents aspects des interactions hôte-pathogènes. L’étude de différents Pattern Recognition Receptors (PRR) autres que les TLR, ainsi que leurs associations… (more)

▼

Nos travaux ont permis d’étudier différents aspects des interactions hôte-pathogènes. L’étude de différents Pattern Recognition Receptors (PRR) autres que les TLR, ainsi que leurs associations a mis en évidence une redondance partielle entre les récepteurs des familles des Scavenger Receptors, lectines de type C et EMR1 in vitro et in vivo dans l’induction de la réponse immunitaire à Mycobacterium tuberculosis. Cette compensation entre les récepteurs contraste avec les rôles indépendants et non redondants des cytokines et de leurs voies associées comme le TNF, l’IL-1R1, L’IFNγR et MyD88, indispensables pour le contrôle de l’infection. Grâce à l’utilisation de nouvelles souris génétiquement modifiées, nous avons pu montrer un rôle minime de la lymphotoxine α dans le contrôle de l’infection par Mycobacterium tuberculosis contrairement au rôle primordial du TNF. Enfin, notre étude s’est poursuivie avec l’analyse de la modulation de la réponse immunitaire de l’hôte par des composants de la paroi des mycobactéries, les PIM. L’élaboration de PIM synthétiques a permis de montrer que ces molécules de faibles poids moléculaires inhibent l’induction des voies TLR4 et TLR2 et possèdent ainsi un potentiel anti-inflammatoire thérapeutique.

In these study, we aimed to investigate different aspects of the host-pathogen interactions. We investigated the involvement of various Pattern Recognition Receptors (PRR) other than TLR, and their associations for the control of M. tuberculosis infection. We highlighted a partial redundancy between members of the Scavenger Receptors family, C-type lectins and EMR1 in response to mycobacteria in vitro and in vivo. This is in sharp contrast with the cytokine pathways like TNF, IL-1R1, IFNγR and MyD88, essentials to control M. tuberculosis infection and which cannot compensate with each other. By using new genetically deficient mice, we showed a limited role for the lymphotoxin α in the control of the infection by Mycobacterium tuberculosis in contrast with the vital role for TNF. Finally, we analysed the modulation of the immune response by mycobacterial cell wall components, PIM. Use of synthetic PIM demonstrated that these small molecules exert an inhibitory activity on TLR4- and TLR2-signaling pathways and may have a therapeutic anti-inflammatory potential.

Advisors/Committee Members: Quesniaux, Valérie (thesis director), Ryffel, Bernhard (thesis director).

Subjects/Keywords: PRR; Scavenger receptors; EMR1; PIM; Pattern Recognition Receptors; Scavenger receptors; EMR1; PIM

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Court Lecuyer, N. (2010). Intéractions hôte-pathogène : rôle des pattern recognition receptors (PRR) dans l'induction de la réponse immunitaire aux mycobactéries et modulation de cette réponse par des composés mycobactériens : Host-pathogen interactions : role of pattern recognition receptors (PRR) for the induction of the host immune response in response to mycobacteria and modulation of this response by mycobacterial components. (Doctoral Dissertation). Université d'Orléans. Retrieved from http://www.theses.fr/2010ORLE2087

Chicago Manual of Style (16^th Edition):

Court Lecuyer, Nathalie. “Intéractions hôte-pathogène : rôle des pattern recognition receptors (PRR) dans l'induction de la réponse immunitaire aux mycobactéries et modulation de cette réponse par des composés mycobactériens : Host-pathogen interactions : role of pattern recognition receptors (PRR) for the induction of the host immune response in response to mycobacteria and modulation of this response by mycobacterial components.” 2010. Doctoral Dissertation, Université d'Orléans. Accessed March 02, 2021. http://www.theses.fr/2010ORLE2087.

MLA Handbook (7^th Edition):

Court Lecuyer, Nathalie. “Intéractions hôte-pathogène : rôle des pattern recognition receptors (PRR) dans l'induction de la réponse immunitaire aux mycobactéries et modulation de cette réponse par des composés mycobactériens : Host-pathogen interactions : role of pattern recognition receptors (PRR) for the induction of the host immune response in response to mycobacteria and modulation of this response by mycobacterial components.” 2010. Web. 02 Mar 2021.

Vancouver:

Court Lecuyer N. Intéractions hôte-pathogène : rôle des pattern recognition receptors (PRR) dans l'induction de la réponse immunitaire aux mycobactéries et modulation de cette réponse par des composés mycobactériens : Host-pathogen interactions : role of pattern recognition receptors (PRR) for the induction of the host immune response in response to mycobacteria and modulation of this response by mycobacterial components. [Internet] [Doctoral dissertation]. Université d'Orléans; 2010. [cited 2021 Mar 02]. Available from: http://www.theses.fr/2010ORLE2087.

Council of Science Editors:

Court Lecuyer N. Intéractions hôte-pathogène : rôle des pattern recognition receptors (PRR) dans l'induction de la réponse immunitaire aux mycobactéries et modulation de cette réponse par des composés mycobactériens : Host-pathogen interactions : role of pattern recognition receptors (PRR) for the induction of the host immune response in response to mycobacteria and modulation of this response by mycobacterial components. [Doctoral Dissertation]. Université d'Orléans; 2010. Available from: http://www.theses.fr/2010ORLE2087

University of Arizona

23. Hild-Petito, Sheri Ann. Distribution of estrogen and progesterone receptors in the primate ovary, with emphasis on subpopulations of cells within the corpus luteum.

Degree: 1988, University of Arizona

URL: http://hdl.handle.net/10150/184485

► Both estradiol and progeterone are proposed autocrine or paracrine regulators of ovarian function in primate species. However, specific receptors for these steroids have not been… (more)

▼ Both estradiol and progeterone are proposed autocrine or paracrine regulators of ovarian function in primate species. However, specific receptors for these steroids have not been localized to individual compartments of the primate ovary. Using immunocytochemical techniques, estradiol receptors were detected in the germinal epithelium, but not other structures, of ovaries obtained from rhesus or cynomolgus monkeys during the follicular and luteal phases of the menstrual cycle. In contrast, progesterone receptors were present in stromal and interstitial tissue, the thecal layers of healthy and atretic follicles, as well as the functional corpus luteum. These results are consistent with the concept of a receptor-mediated role for progesterone, but not estrogen, within the predominant gametogenic and endocrine structures, e.g., the follicle and corpus luteum, of the primate ovary. The recent discovery of distinct cell types in the corpus luteum of domestic ungulates has revised concepts on the control of luteal function in these species. Studies were designed to test the hypothesis that the primate corpus luteum consists of cell subpopulations that differ in physical characteristics, function and regulation. Cells enzymatically-dispersed from the monkey corpus luteum at mid-luteal phase of the menstrual cycle differed in size (diameter) and the presence of the steroidogenic enzyme, 3β-hydroxysteroid dehydrogenase (3β-HSD). Analysis of dispersed cells for forward and 90° light scatter properties by flow cytometry revealed two distinct continua (Cα and Cβ). These continua were isolated using the sorting capabilities of the flow cytometer. Cα contained single cells of ≤ 15 μm and cell clusters; the cells were typically 3β-HSD-negative nonsteroidogenic. Cβ consisted of single cells that increased in size up to 40 μm and were 3β-HSD-positive. Cβ was divided into two regions (R₁ and R₃) and the cells isolated. R₁ cells were ≤ 15 μm whereas R₃ cells were ≥ 20 μm. Basal progesterone and estrogen production by R₃ cells was greater than that produced by R₁ cells (as determined by radioimmunoassay of the incubation media). Relative stimulation of progesterone production by hCG, cAMP or PGE₂ was not different between R₁ and R₃ luteal cells. These results support the hypothesis that the primate corpus luteum consists of distinct cell subpopulations which differ in size and steroidogenic capacity. However, the cell types which secrete progesterone are typically responsive to gonadotropin and PGE₂, possibly via a cAMP-mediated pathway.

Subjects/Keywords: Estrogen – Receptors.; Progesterone – Receptors.; Hormone receptors.

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APA (6^th Edition):

Hild-Petito, S. A. (1988). Distribution of estrogen and progesterone receptors in the primate ovary, with emphasis on subpopulations of cells within the corpus luteum. (Doctoral Dissertation). University of Arizona. Retrieved from http://hdl.handle.net/10150/184485

Chicago Manual of Style (16^th Edition):

Hild-Petito, Sheri Ann. “Distribution of estrogen and progesterone receptors in the primate ovary, with emphasis on subpopulations of cells within the corpus luteum. ” 1988. Doctoral Dissertation, University of Arizona. Accessed March 02, 2021. http://hdl.handle.net/10150/184485.

MLA Handbook (7^th Edition):

Hild-Petito, Sheri Ann. “Distribution of estrogen and progesterone receptors in the primate ovary, with emphasis on subpopulations of cells within the corpus luteum. ” 1988. Web. 02 Mar 2021.

Vancouver:

Hild-Petito SA. Distribution of estrogen and progesterone receptors in the primate ovary, with emphasis on subpopulations of cells within the corpus luteum. [Internet] [Doctoral dissertation]. University of Arizona; 1988. [cited 2021 Mar 02]. Available from: http://hdl.handle.net/10150/184485.

Council of Science Editors:

Hild-Petito SA. Distribution of estrogen and progesterone receptors in the primate ovary, with emphasis on subpopulations of cells within the corpus luteum. [Doctoral Dissertation]. University of Arizona; 1988. Available from: http://hdl.handle.net/10150/184485

Oregon State University

24. Das, Siba Ranjan. Influence of aging and behavioral experience on expression of GluN1 splice variants of the NMDA receptor in prefrontal cortex of mice brain.

Degree: PhD, Molecular and Cellular Biology, 2010, Oregon State University

URL: http://hdl.handle.net/1957/18854

► As the aging population continues to grow the world over, age related complications become more and more apparent among the elderly population. One such complication… (more)

▼ As the aging population continues to grow the world over, age related complications become more and more apparent among the elderly population. One such complication is age associated memory impairment, which makes the elderly more dependent on caregivers early on. NMDA receptors in the brain are important for memory formation, consolidation and retrieval. Expression of NMDA receptors declines with age, which is associated with declines in memory observed during aging. Age-related changes in the protein and mRNA expression of some of the splice forms of the GluN1 (GluN1, NR1) subunit of the NMDA receptor have been seen in mice and rats. The present study was designed to determine whether individual splice forms of the GluN1 subunit of the NMDA receptor within prefrontal / frontal cortical regions contribute to memory deficits during aging and whether experience in learning tasks can influence the expression of the splice forms. mRNA expression of 4 splice forms GluN1[subscript X11], GluN1[subscript X10], GluN1[subscript 0XX] and GluN1[subscript 1XX] (GluN1-1, GluN1-3, GluN1-a and GluN1-b, respectively) and mRNA for all known splice forms (GluN1-pan) were examined by in situ hybridization. mRNA for the C-terminal splice forms, GluN1[subscript X11] (GluN1-1; +C1 and +C2 cassettes) and GluN1[subscript X10] (GluN1-3; +C1 and +C2'), showed significant declines during aging in several brain regions even though overall GluN1-pan mRNA expression was not significantly affected by aging. This work provides evidence that these splice forms are more influenced by aging than the subunit as a whole. There was an increase in the expression of GluN1[subscript 0XX] (GluN1-a; -N1 cassette) splice form in the behaviorally-experienced old mice relative to the younger groups. Old mice with the highest levels of mRNA expression for the GluN1[subscript 0XX] (GluN1-a) splice form in orbital cortex showed the best performances in spatial working and reference memory tasks, but the poorest performances in a cued, associative learning task. These results suggest that the GluN1[subscript 0XX] subunit splice variant may be important for spatial memory performance in the old animals. Protein expression of GluN1 subunits containing C-terminal cassettes C2 or C2' were observed to decline with increasing age, regardless of experience. In middle-age animals, higher expressions of the GluN1 subunit and C2' cassette proteins were associated with good reference memory on initial search. In the aged animals, higher protein expression of GluN1 subunits containing C1 cassettes and the whole population of GluN1 subunits were found to be associated with better performance in the final phase of probe trials but this appeared to be due to perseveration or delays in applying an accurate search. These results provide support for the theory that there is heterogeneity in the effect of aging on the expression of the GluN1 subunits containing different splice cassettes. It also suggests that the GluN1 subunit might be most important for good reference… Advisors/Committee Members: Magnusson, Kathy R. (advisor), Hagen, Tory (committee member).

Subjects/Keywords: NMDA receptor; Methyl aspartate – Receptors

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APA (6^th Edition):

Das, S. R. (2010). Influence of aging and behavioral experience on expression of GluN1 splice variants of the NMDA receptor in prefrontal cortex of mice brain. (Doctoral Dissertation). Oregon State University. Retrieved from http://hdl.handle.net/1957/18854

Chicago Manual of Style (16^th Edition):

Das, Siba Ranjan. “Influence of aging and behavioral experience on expression of GluN1 splice variants of the NMDA receptor in prefrontal cortex of mice brain.” 2010. Doctoral Dissertation, Oregon State University. Accessed March 02, 2021. http://hdl.handle.net/1957/18854.

MLA Handbook (7^th Edition):

Das, Siba Ranjan. “Influence of aging and behavioral experience on expression of GluN1 splice variants of the NMDA receptor in prefrontal cortex of mice brain.” 2010. Web. 02 Mar 2021.

Vancouver:

Das SR. Influence of aging and behavioral experience on expression of GluN1 splice variants of the NMDA receptor in prefrontal cortex of mice brain. [Internet] [Doctoral dissertation]. Oregon State University; 2010. [cited 2021 Mar 02]. Available from: http://hdl.handle.net/1957/18854.

Council of Science Editors:

Das SR. Influence of aging and behavioral experience on expression of GluN1 splice variants of the NMDA receptor in prefrontal cortex of mice brain. [Doctoral Dissertation]. Oregon State University; 2010. Available from: http://hdl.handle.net/1957/18854

Universiteit Utrecht

25. Bink, D.I. Kainate receptors and cognitive enhancement.

Degree: 2011, Universiteit Utrecht

URL: http://dspace.library.uu.nl:8080/handle/1874/193556

► The kainate (KA) receptor family is one of the three ionotropic glutamate receptors (iGluRs) families, consisting of five subunits. The receptors were first discovered by… (more)

Subjects/Keywords: Kainate receptors; Glutamate; LTP; Cognition

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APA (6^th Edition):

Bink, D. I. (2011). Kainate receptors and cognitive enhancement. (Masters Thesis). Universiteit Utrecht. Retrieved from http://dspace.library.uu.nl:8080/handle/1874/193556

Chicago Manual of Style (16^th Edition):

Bink, D I. “Kainate receptors and cognitive enhancement.” 2011. Masters Thesis, Universiteit Utrecht. Accessed March 02, 2021. http://dspace.library.uu.nl:8080/handle/1874/193556.

MLA Handbook (7^th Edition):

Bink, D I. “Kainate receptors and cognitive enhancement.” 2011. Web. 02 Mar 2021.

Vancouver:

Bink DI. Kainate receptors and cognitive enhancement. [Internet] [Masters thesis]. Universiteit Utrecht; 2011. [cited 2021 Mar 02]. Available from: http://dspace.library.uu.nl:8080/handle/1874/193556.

Council of Science Editors:

Bink DI. Kainate receptors and cognitive enhancement. [Masters Thesis]. Universiteit Utrecht; 2011. Available from: http://dspace.library.uu.nl:8080/handle/1874/193556

University of Utah

26. Sonsalla, Patricia Kay. The Roles of D1 and D2 dopamine receptors in mediating methamphetamine-induced changes in monoamine and substance P systems.

Degree: PhD, Pharmacology & Toxicology;, 1985, University of Utah

URL: http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/301/rec/1225

► The amphetamine-like compounds have prominent effects on several neurotransmitter systems within the central nervous system. The administration of multiple doses of these stimulants produces profound… (more)

Subjects/Keywords: Receptors; Dopamine

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APA (6^th Edition):

Sonsalla, P. K. (1985). The Roles of D1 and D2 dopamine receptors in mediating methamphetamine-induced changes in monoamine and substance P systems. (Doctoral Dissertation). University of Utah. Retrieved from http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/301/rec/1225

Chicago Manual of Style (16^th Edition):

Sonsalla, Patricia Kay. “The Roles of D1 and D2 dopamine receptors in mediating methamphetamine-induced changes in monoamine and substance P systems.” 1985. Doctoral Dissertation, University of Utah. Accessed March 02, 2021. http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/301/rec/1225.

MLA Handbook (7^th Edition):

Sonsalla, Patricia Kay. “The Roles of D1 and D2 dopamine receptors in mediating methamphetamine-induced changes in monoamine and substance P systems.” 1985. Web. 02 Mar 2021.

Vancouver:

Sonsalla PK. The Roles of D1 and D2 dopamine receptors in mediating methamphetamine-induced changes in monoamine and substance P systems. [Internet] [Doctoral dissertation]. University of Utah; 1985. [cited 2021 Mar 02]. Available from: http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/301/rec/1225.

Council of Science Editors:

Sonsalla PK. The Roles of D1 and D2 dopamine receptors in mediating methamphetamine-induced changes in monoamine and substance P systems. [Doctoral Dissertation]. University of Utah; 1985. Available from: http://content.lib.utah.edu/cdm/singleitem/collection/etd2/id/301/rec/1225

University of Utah

27. Lin, Ching-Shan. Pharmacokinetic study of uterine progesterone retention;.

Degree: PhD, Pharmaceutics & Pharmaceutical Chemistry;, 1997, University of Utah

URL: http://content.lib.utah.edu/cdm/singleitem/collection/etd1/id/1012/rec/971

► Tritium-labeled progesterone was administered to mature female rate in the proestrous stage of three different routes, gastric intubation, subcutaneous injection, and uterine intraluminal instillation, to… (more)

▼ Tritium-labeled progesterone was administered to mature female rate in the proestrous stage of three different routes, gastric intubation, subcutaneous injection, and uterine intraluminal instillation, to study the kinetics involved in the uptake and retention of radioactivity by the uterus and various other tissues. Progesterone was retained at a much higher level and for a more prolonged period in the rat uterus after uterine intraluminal instillation. Progesterone bioavailability to the uterus was 45 times higher by uterine intraluminal instillation than by either gastric intubation or subcutaneous injection. Progesterone absorption by the rat endometrium was extremely fast. The observed biphasic decrease of radioactivity from the uterine tissue was explained adequately by a pharmacokinetic model in which progesterone is assumed to be present in two compartments within the uterine tissue. The pharmacokinetic parameters showed that the progesterone biological half-life in the uterine tissue during the alpha-phase was about 6.5 min, while that in the beta-phase was about 230 min. Tritium-labeled progesterone was perfused through the uterine luminal cavity of the rat until a steady state was reached. The radioactivity was found to exist at a mush higher concentration in the uterine tissue than many other tissues studies. The amount of radioactivity retained by the uterine tissue under constant perfusion was adequately described by a pharmacokinetic equation derived from a two-compartment open model. The amount of progesterone residing in the uterine tissue may, thus, be predicted from this equation using the predetermined pharmacokinetic parameters. At the steady state, the observed experimental values were in close approximation with the predicted values. A cyclic change in the uptake and retention of progesterone by uterine tissues was observed with rats in different stages of estrous cycle. Long-term insertion of the “Uterine Progesterone System,” however, did not cause any significant change in the uterine capacity for either the absorption or the retention of progesterone administered by the direct uterine intraluminal route. The levels of the nuclear receptors for estradiol-17beta and progesterone in the uterine tissues of rats were measured by a 3H-steroid exchange method in which the specific 3H-steroid binding sites were estimated after the addition of an excess amount of the same but nonlabeled steroid. A similar procedure was used for the quantification of the progesterone cytosol receptor in rat uterine tissue. The level of the uterine estradiol-17beta cytosol receptor was determined from the amount of 8S complex obtained after a sucrose gradient centrifugation. The highest amounts of estradiol-17beta and progesterone receptors were found in uterine nuclei and cytosol of animals in proestrous, followed by diestrus, estrus, and metestrus in that order. No significant changes in the levels of either nuclear or cytosol receptors for both hormones were observed in the uterine tissues of rats inserted “Uterine…

Subjects/Keywords: Pharmacokinetics; Receptors

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APA (6^th Edition):

Lin, C. (1997). Pharmacokinetic study of uterine progesterone retention;. (Doctoral Dissertation). University of Utah. Retrieved from http://content.lib.utah.edu/cdm/singleitem/collection/etd1/id/1012/rec/971

Chicago Manual of Style (16^th Edition):

Lin, Ching-Shan. “Pharmacokinetic study of uterine progesterone retention;.” 1997. Doctoral Dissertation, University of Utah. Accessed March 02, 2021. http://content.lib.utah.edu/cdm/singleitem/collection/etd1/id/1012/rec/971.

MLA Handbook (7^th Edition):

Lin, Ching-Shan. “Pharmacokinetic study of uterine progesterone retention;.” 1997. Web. 02 Mar 2021.

Vancouver:

Lin C. Pharmacokinetic study of uterine progesterone retention;. [Internet] [Doctoral dissertation]. University of Utah; 1997. [cited 2021 Mar 02]. Available from: http://content.lib.utah.edu/cdm/singleitem/collection/etd1/id/1012/rec/971.

Council of Science Editors:

Lin C. Pharmacokinetic study of uterine progesterone retention;. [Doctoral Dissertation]. University of Utah; 1997. Available from: http://content.lib.utah.edu/cdm/singleitem/collection/etd1/id/1012/rec/971

28. Mailhac, Camille. Développement d’outils pour l'étude de la signalisation médiée par les récepteurs couplés aux protéines G, basés sur l'utilisation d'anticorps à domaine unique de lama : Development of tools for the study of G protein-coupled receptor-mediated signaling based on the use of lama single domain antibodies.

Degree: Docteur es, Biologie. Immunologie, 2017, Aix Marseille Université

URL: http://www.theses.fr/2017AIXM0405

►

L'objectif principal de ma thèse était de développer de nouvelles technologies et des outils pour l’étude de l’activation des récepteurs couplés aux protéines G (GPCR).À… (more)

▼

L'objectif principal de ma thèse était de développer de nouvelles technologies et des outils pour l’étude de l’activation des récepteurs couplés aux protéines G (GPCR).À la surface de la cellule se trouve une multitude de récepteurs qui jouent un rôle critique dans la communication cellule-cellule, dont les GPCR, une famille de récepteur utilisant les protéines G intracellulaires pour transmettre leurs signaux. Le ciblage de ces récepteurs à des fins thérapeutique est innovant et très prometteur. Mais à ce jour seuls quelques médicaments ciblant les GPCR ont été mis sur le marché, en partie en raison d'un manque d'outils permettant le suivi de leur action sur les cellules natives.L’objectif de cette thèse est donc de développer des tests simples pour suivre l’activation de n’importe quel GPCR. Pour développer ce type de test, nous avons décidé d'utiliser des fragments d'anticorps appelés nanobodies. Les anticorps sont des protéines du sang produites en réponse à un antigène spécifique qui sont capable de le neutraliser. Les nanobodies correspondent au domaine variable de certains anticorps de camélidés. En raison de leur faible taille (13 kDa) et de leur site de liaison à l'antigène réduit, les nanobodies se lient souvent à des cavités et présentent une grande sensibilité aux changements de conformation de l'antigène.

The main objective of my thesis was to develop technologies and tools to study activation of G protein-coupled receptors (GPCRs).The cell surface is displaying a multitude of receptors, who play critical roles in cell-cell communication. Among them, GPCRs represent a large family relying on the use of intracellular G proteins for their signaling. Targeting these receptors for therapies is very promising and innovative. So far, only few new drugs have been put on the market, partly due to a lack of tools enabling the follow-up of their action on native cells.The aim of this thesis is thus to develop simple assays to study activation of any GPCRs. To develop this kind of test, we used antibody fragments called nanobodies. Antibodies are blood protein produced in response to and counteracting a specific antigen. Nanobodies correspond to antibody fragments derived from the variable domain of a special class of camelid antibodies. Because of their small size (13 kDa) and reduced antigen binding site, nanobodies often bind cavities and show a high sensitivity to antigen conformational changes.

Advisors/Committee Members: Chames, Patrick (thesis director).

Subjects/Keywords: RCPG; G protein coupled receptors

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APA (6^th Edition):

Mailhac, C. (2017). Développement d’outils pour l'étude de la signalisation médiée par les récepteurs couplés aux protéines G, basés sur l'utilisation d'anticorps à domaine unique de lama : Development of tools for the study of G protein-coupled receptor-mediated signaling based on the use of lama single domain antibodies. (Doctoral Dissertation). Aix Marseille Université. Retrieved from http://www.theses.fr/2017AIXM0405

Chicago Manual of Style (16^th Edition):

Mailhac, Camille. “Développement d’outils pour l'étude de la signalisation médiée par les récepteurs couplés aux protéines G, basés sur l'utilisation d'anticorps à domaine unique de lama : Development of tools for the study of G protein-coupled receptor-mediated signaling based on the use of lama single domain antibodies.” 2017. Doctoral Dissertation, Aix Marseille Université. Accessed March 02, 2021. http://www.theses.fr/2017AIXM0405.

MLA Handbook (7^th Edition):

Mailhac, Camille. “Développement d’outils pour l'étude de la signalisation médiée par les récepteurs couplés aux protéines G, basés sur l'utilisation d'anticorps à domaine unique de lama : Development of tools for the study of G protein-coupled receptor-mediated signaling based on the use of lama single domain antibodies.” 2017. Web. 02 Mar 2021.

Vancouver:

Mailhac C. Développement d’outils pour l'étude de la signalisation médiée par les récepteurs couplés aux protéines G, basés sur l'utilisation d'anticorps à domaine unique de lama : Development of tools for the study of G protein-coupled receptor-mediated signaling based on the use of lama single domain antibodies. [Internet] [Doctoral dissertation]. Aix Marseille Université 2017. [cited 2021 Mar 02]. Available from: http://www.theses.fr/2017AIXM0405.

Council of Science Editors:

Mailhac C. Développement d’outils pour l'étude de la signalisation médiée par les récepteurs couplés aux protéines G, basés sur l'utilisation d'anticorps à domaine unique de lama : Development of tools for the study of G protein-coupled receptor-mediated signaling based on the use of lama single domain antibodies. [Doctoral Dissertation]. Aix Marseille Université 2017. Available from: http://www.theses.fr/2017AIXM0405

University of Hong Kong

29. Lui, Wan, Thomas. Biochemical events induced by the specific kappa-opioid receptor agonist, U50488H.

Degree: 2007, University of Hong Kong

URL: http://hdl.handle.net/10722/131320

Subjects/Keywords: Opioids - Receptors.

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APA (6^th Edition):

Lui, Wan, T. (2007). Biochemical events induced by the specific kappa-opioid receptor agonist, U50488H. (Thesis). University of Hong Kong. Retrieved from http://hdl.handle.net/10722/131320

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Lui, Wan, Thomas. “Biochemical events induced by the specific kappa-opioid receptor agonist, U50488H.” 2007. Thesis, University of Hong Kong. Accessed March 02, 2021. http://hdl.handle.net/10722/131320.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Lui, Wan, Thomas. “Biochemical events induced by the specific kappa-opioid receptor agonist, U50488H.” 2007. Web. 02 Mar 2021.

Vancouver:

Lui, Wan T. Biochemical events induced by the specific kappa-opioid receptor agonist, U50488H. [Internet] [Thesis]. University of Hong Kong; 2007. [cited 2021 Mar 02]. Available from: http://hdl.handle.net/10722/131320.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Lui, Wan T. Biochemical events induced by the specific kappa-opioid receptor agonist, U50488H. [Thesis]. University of Hong Kong; 2007. Available from: http://hdl.handle.net/10722/131320

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

University of Rochester

30. Saperstein, Sara C. Modulation of TNF-α-mediated acute lung inflammation : a role for IL-1β and soluble TNF receptors.

Degree: PhD, 2009, University of Rochester

URL: http://hdl.handle.net/1802/8631

► Tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) are key mediators of numerous lung inflammatory diseases. Induced by similar stimuli, in many cell types IL-1β modifies… (more)

▼ Tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) are key mediators of numerous lung inflammatory diseases. Induced by similar stimuli, in many cell types IL-1β modifies expression and solubilization of the two TNF receptors, TNFR1 and TNFR2. These proteins are cleaved from the cell surface primarily by the metalloprotease TNF-α converting enzyme (TACE) generating soluble forms still capable of binding TNF-α. Investigators postulate that the shed receptors either act as natural antagonists or as a TNF-α reservoir extending the half-life of the cognate ligand. Based on these observations, IL-1β effects on lung TNF-α-mediated inflammatory responses, as well as on TNF receptor expression and shedding, both in vitro and in vivo were investigated. Finally, the roles of the two soluble TNF receptors (sTNFR) on altering ligand-induced inflammation and cytotoxicity were analyzed. Studies utilizing an in vitro culture system, murine epithelial type II-like cells (MLE-15), and transgenic IL-1β null mice showed that the interleukin enhances acute, TNF-α-mediated pulmonary inflammatory processes. In vitro, IL-1β induced MLE-15 surface TNF receptor expression which correlated with increased mRNA levels and protein secretion of the two neutrophil chemoattractants macrophage inflammatory protein (MIP-2) and KC following TNF-α exposure. Further studies investigating the regulation of the two receptors demonstrated a counter-regulatory role for each; TNFR1 expression was necessary for interleukin-mediated TNFR2 shedding and surface expression and vice a versa. In vivo studies corroborated these findings. IL-1β KO mice instilled with TNF-α had decreased neutrophil influx measured in the lavage fluid of the lung. This correlated with a decrease in lavage sTNFR1 and MIP-2, although sTNFR2 and KC were unaffected. Finally, at a ratio of approximately 1:1 to 1:25, sTNFR1:sTNFR2 functioned as TNF-α antagonists in vitro. Taken together, the studies in this thesis suggest that IL-1β modulates TNF-α-mediated inflammatory lung diseases by altering TNF receptor shedding and expression in epithelial cells, resulting in altered chemoattractant production in response to TNF-α, hence augmenting recruitment of inflammatory cells.

Subjects/Keywords: Inflammation; Receptors

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APA (6^th Edition):

Saperstein, S. C. (2009). Modulation of TNF-α-mediated acute lung inflammation : a role for IL-1β and soluble TNF receptors. (Doctoral Dissertation). University of Rochester. Retrieved from http://hdl.handle.net/1802/8631

Chicago Manual of Style (16^th Edition):

Saperstein, Sara C. “Modulation of TNF-α-mediated acute lung inflammation : a role for IL-1β and soluble TNF receptors.” 2009. Doctoral Dissertation, University of Rochester. Accessed March 02, 2021. http://hdl.handle.net/1802/8631.

MLA Handbook (7^th Edition):

Saperstein, Sara C. “Modulation of TNF-α-mediated acute lung inflammation : a role for IL-1β and soluble TNF receptors.” 2009. Web. 02 Mar 2021.

Vancouver:

Saperstein SC. Modulation of TNF-α-mediated acute lung inflammation : a role for IL-1β and soluble TNF receptors. [Internet] [Doctoral dissertation]. University of Rochester; 2009. [cited 2021 Mar 02]. Available from: http://hdl.handle.net/1802/8631.

Council of Science Editors:

Saperstein SC. Modulation of TNF-α-mediated acute lung inflammation : a role for IL-1β and soluble TNF receptors. [Doctoral Dissertation]. University of Rochester; 2009. Available from: http://hdl.handle.net/1802/8631

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Open Access Theses and Dissertations