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A Historical Perspective of G Protein-Coupled Receptor Structural Biology

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Advances in Membrane Proteins

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Abstract

G protein-coupled receptors (GPCRs) are the largest family of integral membrane proteins. With more than 800 members, they play an important role in mediating cell signaling across the cytoplasmic membrane to activate downstream proteins such as G proteins and β-arrestins. The first GPCR crystal structure determined was bovine rhodopsin in 2000. Since 2007, there have been more than 300 crystal structures and 12 cryo-EM structures published, while those numbers keep growing. This article is aimed at providing some historical perspectives of this so-called golden age of GPCR structural biology, as well as some new insights from the structures into the mechanism of GPCR signaling at molecular and atomic levels.

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Acknowledgments

This work is supported by National Key Research and Development Program of China (2018YFC1004704 and 2017YFC1001303), NSFC-CAS Joint Fund for Research Based on Large-Scale Scientific Facilities (U1632132), and NSFC General Program (31670849). Given the space limitation of the article, the authors regret the omission of many excellent publications on the subject matter.

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  1. Department of Orthopaedics and Institute of Precision Medicine, Shanghai Key Laboratory of Orthopaedic Implant, Shanghai Ninth People’s Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China

    Yang Chen, Ying Xia & Yu Cao

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  1. Yang Chen
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  2. Ying Xia
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  3. Yu Cao
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Correspondence to Yu Cao .

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  1. Department of Orthopaedics and Institute of Precision Medicine, Shanghai Key Laboratory of Orthopaedic Implant, Shanghai Ninth People’s Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China

    Yu Cao

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Chen, Y., Xia, Y., Cao, Y. (2019). A Historical Perspective of G Protein-Coupled Receptor Structural Biology. In: Cao, Y. (eds) Advances in Membrane Proteins. Springer, Singapore. https://doi.org/10.1007/978-981-13-9077-7_2

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