In vitro expression and analysis of the 826 human G protein-coupled receptors
Received date: 26 Feb 2016
Accepted date: 09 Mar 2016
Published date: 27 May 2016
Copyright
G protein-coupled receptors (GPCRs) are involved in all humanphysiological systems where they are responsible for transducing extracellular signals into cells. GPCRs signal in response to a diverse array of stimuli including light, hormones, and lipids, where these signals affect downstream cascades to impact both health and disease states. Yet, despite their importance as therapeutic targets, detailed molecular structures of only 30 GPCRs have been determined to date. A key challenge to their structure determination is adequate protein expression. Here we report the quantification of protein expression in an insect cell expression system for all 826humanGPCRs using two different fusion constructs. Expression characteristics are analyzed in aggregate and among each of the five distinct subfamilies. These data can be used to identify trends related to GPCR expression between different fusion constructs and between different GPCR families, and to prioritize lead candidates for future structure determination feasibility.
Xuechen Lv , Junlin Liu , Qiaoyun Shi , Qiwen Tan , Dong Wu , John J. Skinner , Angela L. Walker , Lixia Zhao , Xiangxiang Gu , Na Chen , Lu Xue , Pei Si , Lu Zhang , Zeshi Wang , Vsevolod Katritch , Zhi-jie Liu , Raymond C. Stevens . In vitro expression and analysis of the 826 human G protein-coupled receptors[J]. Protein & Cell, 2016 , 7(5) : 325 -337 . DOI: 10.1007/s13238-016-0263-8
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