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In vitro expression and analysis of the 826 human G protein-coupled receptors |
Xuechen Lv1,Junlin Liu1,Qiaoyun Shi1,Qiwen Tan1,Dong Wu1,John J. Skinner1,Angela L. Walker2,Lixia Zhao1,Xiangxiang Gu1,Na Chen1,Lu Xue1,Pei Si1,Lu Zhang1,Zeshi Wang1,Vsevolod Katritch2,Zhi-jie Liu1,Raymond C. Stevens1,*( ) |
1. iHuman Institute, ShanghaiTech University, Shanghai 201210, China 2. Department of Biological Sciences, Bridge Institute, University of Southern California, Los Angeles, CA 90089, USA |
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Abstract 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.
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| Keywords
G protein-coupled receptors
insect
protein expression
surface expression analysis
fusion construct
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Corresponding Author(s):
Raymond C. Stevens
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Issue Date: 27 May 2016
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