Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 14 of 14 for “"Receptors, G-Protein-Coupled"”.
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Role of TGR5 in Bile Acid Metabolism
TGR5 is a G protein-coupled bile acid receptor present in various tissues in the body. Its agonism increases energy expenditure and lowers blood glucose. Thus, it is an attractive drug target for treating human metabolic disease. However, TGR5 is highly expressed in the gallbladder, where its …
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In vivo identification of drug therapeutics for nemaline myopathy
… key mechanisms of action including adrenergic receptors, cholinergic receptors, histamine receptors, G-protein coupled receptors/ion channels, nuclear receptors, tyrosine kinase receptors, and other non-receptor enzyme inhibitors. To test the efficacy of these compounds in a mammalian system, …
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G Protein and Androgen Signaling in Ovarian Function
… have implicated a constitutively activated Gas-coupled receptor, G protein-coupled receptor 3 (GPR3), as one of the molecules responsible for maintaining meiotic arrest in mouse oocytes. Here, we characterized the signaling and functional properties of GPR3 by using the more amenable model …
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Short Chain Fatty Acids Signaling through the G Protein-Coupled Receptor GPR41 in the Intestine.
… SCFAs have been shown to be ligands fortwo G protein-coupled receptors (GPCRs), Gpr41 and Gpr43. We show that Gpr41 is expressed in the intestinal enteroendocrine cells. The localization of Gpr41 to enteroendocrine cells suggests that SCFAs signaling through Gpr41 induces the enteroendocrine …
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Chemically Based Interrogation of Smoothened, a Proto-Oncogenic Component of the Hedgehog Signal Transduction Pathway
… to misactivation of the seven transmembrane oncoprotein, Smoothened (Smo). Thus, Smo is a high priority therapeutic target in Hh-associated cancers including basal cell carcinoma (BCC) and medulloblastoma. While a Smo antagonist is now approved for the management of BCC, therapeutic strategies …
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Rgs16 is a Pancreatic Reporter of Chronic Hyperglycemia in Diabetes
… insulin release for type 2 diabetics. G-protein coupled receptors (GPCR) represent the largest non-antibiotic drug targets and several family members are expressed in beta cells. Regulators of G-protein Signaling (RGS) proteins are feedback regulators of GPCRs. Their expression can be …
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Structural Studies of Integral Membrane Proteins Involved in GPCR Signaling and Sterol Homeostasis
Membrane proteins are crucial molecules for cellular survival, and can take on multiple and diverse roles within the native membrane. In this dissertation, I will detail my efforts to understand and study two different types of membrane proteins. First, I will discuss my research developing and …
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Crosstalk Signaling Between cAMP and mTORC1
… to regulate anabolic and catabolic processes. G-protein-coupled receptors (GPCRs) paired to Gs proteins increase cyclic adenosine 3'5' monophosphate (cAMP) to activate protein kinase A (PKA), which phosphorylates Raptor at Ser 791 resulting in potent mTORC1 inhibition. We identified a novel …
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Molecular mechanism of ligand induced regulation of cannabinoid receptors
Submission published under a 24 month embargo labeled 'Closed Access', the embargo will last until 2025-12-01
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Constitutive activity in orphan G protein coupled receptors
… constitutive signaling among orphan class-A G protein coupled receptors (GPCRs). These receptors translate extracellular signals via conformational change into intracellular activation of different G proteins and subsequent second messenger synthesis. These small molecules regulate cellular …
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FUNCTIONAL SELECTIVITY DOWNSTREAM OF Gαi/o-COUPLED RECEPTORS
G protein-coupled receptors (GPCRs) are drug targets that often activate multiple signaling pathways. The multiple GPCR responses provide opportunities for biased or functionally selective ligands to preferentially modulate one signaling pathway over another. Studies with several GPCRs have …
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Signal Transduction Mechanisms Mediating the Regulation of Vascular G Protein-Coupled Receptors
… signaling mechanisms. Among the broad network of receptors and signaling molecules regulating blood vessel reactivity, members of the G protein-coupled receptor (GPCR) family are known to play a central role. GPCR activity represents a delicate, but coordinated balance between molecular mechanisms …
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Investigating the molecular pharmacology of class A and B G protein-coupled receptors
G protein-coupled receptors (GPCRs) possess an inherent ability to bind to an extremely diverse range of ligands and activate multiple downstream signalling pathways. It is becomingly increasingly evident, however, that for many GPCRs, the exact downstream signalling cascade(s), and the extent of …
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Activation mechanisms of non-class A G protein-coupled receptors
G protein-coupled receptors are central to mediating homeostasis across a plethora of biochemical signaling pathways across the entire body and are one of the most important classes of drug targets. While the majority of the recent literature on GPCRs focuses on Class A GPCRs, the structural and …