Book Chapter10.1016/B978-0-12-394440-5.00004-8
Arrestins: role in the desensitization, sequestration, and vesicular trafficking of G protein-coupled receptors.
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TL;DR: This chapter summarizes the current understanding of the β-arrestin family's unique ability to control the kinetics as well as the extent of GPCR activity at the level of desensitization, sequestration, and subsequent intracellular trafficking.
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Abstract: Over the years, β-arrestins have emerged as multifunctional molecular scaffolding proteins regulating almost every imaginable G protein-coupled receptor (GPCR) function. Originally discovered as GPCR-desensitizing molecules, they have been shown to also serve as important regulators of GPCR signaling, sequestration, and vesicular trafficking. This broad functional role implicates β-arrestins as key regulatory proteins for cellular function. Hence, this chapter summarizes the current understanding of the β-arrestin family's unique ability to control the kinetics as well as the extent of GPCR activity at the level of desensitization, sequestration, and subsequent intracellular trafficking.
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Citations
Deletion of β-Arrestin2 in Mice Limited Pancreatic β-Cell Expansion under Metabolic Stress through Activation of the JNK Pathway
Ziwei Lin,Yu Zhao,Lige Song,Kaida Mu,Mingliang Zhang,Hongxia Liu,Xiaowen Li,Jian Zhao,Chen Wang,Weiping Jia +9 more
TL;DR: βarr2 plays roles in regulation of pancreatic β-cell mass through the modulation of cell cycle regulatory genes and the inhibition of JNK activation induced by glucolipotoxity, which implicates a role for βarr2 in the development of type 2 diabetes.
Roles of M3 receptor in the effect of penehyclidine hydrochloride upregulated beta-arrestin-1 expression in LPS-stimulated HPMVEC.
TL;DR: The results indicate that M3 receptor plays an important role in pulmonary microvascular endothelial barrier function, and knock-out of M3 receptors could attenuate LPS-induced pulmonary microVascular endothelium injury.
2
Strategies for G-protein coupled receptor deorphanization
Sorin Tunaru
- 01 Jul 2017
TL;DR: Although GPCRs are the most prominent drug target, almost 140 genes in human genome still encode receptors for which neither biological roles nor endogenous ligands have been identifi ed, termed orphan GPCR (oGPCRs) and are under intense scientific investigations by the pharma industry and academia to discover ligands and thus to determine their contribution to pathophysiology.
1
The Functional Role of the Conformational Changes in Arrestin Upon Activation
Zhao Yang,Fan Yang,Anthony Nguen,Chuan Liu,Amy Lin,Thomas Joseph CahillIII,Jin-Peng Sun +6 more
- 01 Jan 2017
TL;DR: The current knowledge of the structural features of arrestins that underlie selective arrestin-mediated signaling are reviewed and recent breakthroughs in the functional correlation of the conformational changes in arrestin to downstream effector molecules were highlighted.
1
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•Journal Article
Evolving Concepts in G Protein-Coupled Receptor Endocytosis: The Role in Receptor Desensitization and Signaling
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