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A G Protein-biased Designer G Protein-coupled Receptor Useful for Studying the Physiological Relevance of Gq/11-dependent Signaling Pathways.

J. Biol. Chem.. 2016-05; 
HuJianxin,SternMatthew,GimenezLuis E,WankaLizzy,ZhuLu,RossiMario,MeisterJaroslawna,InoueAsuka,Beck-SickingerAnnette G,GurevichVsevolod V,WessJü
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摘要

Designerreceptorsexclusivelyactivated by adesignerdrug (DREADDs) are clozapine-N-oxide-sensitive designer G protein-coupled receptors (GPCRs) that have emerged as powerful novel chemogenetic tools to study the physiological relevance of GPCR signaling pathways in specific cell types or tissues. Like endogenous GPCRs, clozapine-N-oxide-activated DREADDs do not only activate heterotrimeric G proteins but can also trigger β-arrestin-dependent (G protein-independent) signaling. To dissect the relative physiological relevance of G protein-mediatedversusβ-arrestin-mediated signaling in different cell types or physiological processes, the availability of G protein- and β-arrestin-biased DREADDs would be highly ... More

关键词

7-helix receptor,DREADD,G protein,G protein-coupled receptor (GPCR),arrestin,biased signaling,cell signa