title: In vitro expression and analysis of the 826 human G protein-coupled receptors.
abstract: G protein-coupled receptors (GPCRs) are involved in all human physiological 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 826 human GPCRs 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.
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Xuechen
authors.initials: X
authors.lastname: Lv
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Junlin
authors.initials: J
authors.lastname: Liu
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Qiaoyun
authors.initials: Q
authors.lastname: Shi
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Qiwen
authors.initials: Q
authors.lastname: Tan
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Dong
authors.initials: D
authors.lastname: Wu
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: John J
authors.initials: JJ
authors.lastname: Skinner
authors.affiliation: Department of Biological Sciences, Bridge Institute, University of Southern California, Los Angeles, CA, 90089, USA.
authors.forename: Angela L
authors.initials: AL
authors.lastname: Walker
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Lixia
authors.initials: L
authors.lastname: Zhao
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Xiangxiang
authors.initials: X
authors.lastname: Gu
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Na
authors.initials: N
authors.lastname: Chen
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Lu
authors.initials: L
authors.lastname: Xue
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Pei
authors.initials: P
authors.lastname: Si
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Lu
authors.initials: L
authors.lastname: Zhang
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Zeshi
authors.initials: Z
authors.lastname: Wang
authors.affiliation: Department of Biological Sciences, Bridge Institute, University of Southern California, Los Angeles, CA, 90089, USA.
authors.forename: Vsevolod
authors.initials: V
authors.lastname: Katritch
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.
authors.forename: Zhi-Jie
authors.initials: ZJ
authors.lastname: Liu
authors.affiliation: iHuman Institute, ShanghaiTech University, Shanghai, 201210, China. stevens@shanghaitech.edu.cn.
authors.forename: Raymond C
authors.initials: RC
authors.lastname: Stevens
mesh_terms: D000818:Animals; D019295:Computational Biology; D018360:Crystallography, X-Ray; D015870:Gene Expression; D006801:Humans; D010957:Plasmids / Q000235:genetics / Q000378:metabolism; D000072417:Protein Domains; D018342:Receptors, Adrenergic, beta-1; D043562:Receptors, G-Protein-Coupled / Q000145:classification / Q000235:genetics / Q000378:metabolism*; D018035:Receptors, Odorant / Q000378:metabolism; D018047:Receptors, Purinergic P1 / Q000235:genetics / Q000378:metabolism; D061987:Sf9 Cells; D018411:Spodoptera
chemical_list: D018342:Receptors, Adrenergic, beta-1; D043562:Receptors, G-Protein-Coupled; D018035:Receptors, Odorant; D018047:Receptors, Purinergic P1
keywords: G protein-coupled receptors; fusion construct; insect; protein expression; surface expression analysis