Regulation of GPCR activity, trafficking and localization by GPCR-interacting proteins
نویسندگان
چکیده
منابع مشابه
GPCR-interacting proteins (GIPs): nature and functions.
The simplistic idea that seven transmembrane receptors are single monomeric proteins that interact with heterotrimeric G-proteins after agonist binding is definitively out of date. Indeed, GPCRs (G-protein-coupled receptors) are part of multiprotein networks organized around scaffolding proteins. These GIPs (GPCR-interacting proteins) are either transmembrane or cytosolic proteins. Proteomic ap...
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G protein-coupled receptors (GPCRs), major targets of drug discovery, are organized in dimeric and/or oligomeric clusters. The minimal oligomeric unit, the dimer, is composed of two protomers, which can behave differently within the dimer. Several examples of GPCR asymmetry within dimers at the level of ligand binding, ligandpromoted conformational changes, conformational changes within transme...
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Many GPCRs are able to activate multiple distinct signaling pathways, and these may include biochemical cascades activated via either heterotrimeric G proteins or by β-arrestins. The relative potencies and/or efficacies among a series of agonists that act on a common receptor can vary depending upon which signaling pathway is being activated. This phenomenon is known as biased signaling or func...
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Beta-arrestins are signaling adaptors that bind to agonist-occupied G proteincoupled receptors (GPCRs) and target them for endocytosis; however, the mechanisms regulating receptor/!-arrestin complexes and trafficking in endosomes, remain ill defined. Here we show, in live cells, differential dynamic regulation of endosomal bradykinin B2 receptor (B2R) complexes with either !arrestin-1 or -2. We...
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G protein-coupled receptors (GPCRs) have critical roles in various physiological and pathophysiological processes, and more than 40% of marketed drugs target GPCRs. Although the canonical downstream target of an agonist-activated GPCR is a G protein heterotrimer; there is a growing body of evidence suggesting that other signaling molecules interact, directly or indirectly, with GPCRs. However, ...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2012
ISSN: 0007-1188
DOI: 10.1111/j.1476-5381.2011.01552.x