G protein-coupled receptors: structure- and function-based drug discovery

Dehua Yang; Qingtong Zhou; Viktorija Labroska; Shanshan Qin; Sanaz Darbalaei; Yiran Wu; Elita Yuliantie; Linshan Xie; Houchao Tao; Jianjun Cheng; Qing Liu; Suwen Zhao; Wenqing Shui; Yi Jiang; Ming-Wei Wang

doi:10.1038/s41392-020-00435-w

G protein-coupled receptors: structure- and function-based drug discovery

Signal Transduct Target Ther. 2021 Jan 8;6(1):7. doi: 10.1038/s41392-020-00435-w.

Authors

Dehua Yang^{1

2}, Qingtong Zhou³, Viktorija Labroska^{1

4}, Shanshan Qin⁵, Sanaz Darbalaei^{1

4}, Yiran Wu⁵, Elita Yuliantie^{1

4}, Linshan Xie^{5

6}, Houchao Tao⁵, Jianjun Cheng⁵, Qing Liu^{1

2}, Suwen Zhao^{5

6}, Wenqing Shui^{7

8}, Yi Jiang⁹, Ming-Wei Wang^{10

11

12

13

14

15}

Affiliations

¹ The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 201203, Shanghai, China.
² The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 201203, Shanghai, China.
³ School of Basic Medical Sciences, Fudan University, 200032, Shanghai, China.
⁴ University of Chinese Academy of Sciences, 100049, Beijing, China.
⁵ iHuman Institute, ShanghaiTech University, 201210, Shanghai, China.
⁶ School of Life Science and Technology, ShanghaiTech University, 201210, Shanghai, China.
⁷ iHuman Institute, ShanghaiTech University, 201210, Shanghai, China. shuiwq@shanghaitech.edu.cn.
⁸ School of Life Science and Technology, ShanghaiTech University, 201210, Shanghai, China. shuiwq@shanghaitech.edu.cn.
⁹ The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 201203, Shanghai, China. yijiang@simm.ac.cn.
¹⁰ The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 201203, Shanghai, China. mwwang@simm.ac.cn.
¹¹ The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 201203, Shanghai, China. mwwang@simm.ac.cn.
¹² School of Basic Medical Sciences, Fudan University, 200032, Shanghai, China. mwwang@simm.ac.cn.
¹³ University of Chinese Academy of Sciences, 100049, Beijing, China. mwwang@simm.ac.cn.
¹⁴ School of Life Science and Technology, ShanghaiTech University, 201210, Shanghai, China. mwwang@simm.ac.cn.
¹⁵ School of Pharmacy, Fudan University, 201203, Shanghai, China. mwwang@simm.ac.cn.

Abstract

As one of the most successful therapeutic target families, G protein-coupled receptors (GPCRs) have experienced a transformation from random ligand screening to knowledge-driven drug design. We are eye-witnessing tremendous progresses made recently in the understanding of their structure-function relationships that facilitated drug development at an unprecedented pace. This article intends to provide a comprehensive overview of this important field to a broader readership that shares some common interests in drug discovery.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Animals
Drug Design*
Drug Discovery*
Humans
Receptors, G-Protein-Coupled* / antagonists & inhibitors
Receptors, G-Protein-Coupled* / chemistry
Structure-Activity Relationship

Substances

Receptors, G-Protein-Coupled