Functional Selectivity in GPCR Heterocomplexes
نویسندگان
چکیده
منابع مشابه
Functional selectivity of GPCR ligand stereoisomers: new pharmacological opportunities.
It is now well established that any given ligand for a G-protein-couple receptor (GPCR) does not simply possess a single defined efficacy. Rather, a ligand possesses multiple efficacies, depending on the specific down-stream signal transduction pathway analyzed. This diversity may be based on ligand-specific GPCR conformations and is often referred to as "functional selectivity." It has been kn...
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This review focuses on the existence and function of multiple endogenous agonists of the somatostatin and opioid receptors with an emphasis on their expression in the gastrointestinal tract. These agonists generally arise from the proteolytic cleavage of prepropeptides during peptide maturation or from degradation of peptides by extracellular or intracellular endopeptidases. In other examples, ...
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National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, Department of Health and Human Services, Baltimore, Maryland (X.G., H.Y., N.S.C., M.S.S., S.K-B., Y.T.N., S.F.); Centro de Investigación Biomédica en Red sobre Enfermedades Neurodegenerativas and Department of Biochemistry and Molecular Biology, Faculty of Biology, University of Barcelona, Barcelona, S...
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Here we present a new method that combines protein complementation with resonance energy transfer to study conformational changes in response to activation of a defined G protein-coupled receptor heteromer, and we apply the approach to the putative dopamine D1-D2 receptor heteromer. Remarkably, the potency of the D2 dopamine receptor (D2R) agonist R-(-)-10,11-dihydroxy-N-n-propylnoraporphine (N...
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ژورنال
عنوان ژورنال: Mini-Reviews in Medicinal Chemistry
سال: 2012
ISSN: 1389-5575
DOI: 10.2174/138955712800959152