Chinese Journal of Nature ›› 2021, Vol. 43 ›› Issue (1): 45-52.doi: 10.3969/j.issn.0253-9608.2021.01.007

• Review Article • Previous Articles     Next Articles

Common activation mechanism of GPCR

ZHOU Qingtong, DAI Zhizhuo②③, ZHAO Suwen②③   

  1. ①School of Basic Medical Sciences, Fudan University, Shanghai 200032, China; ②iHuman Institute, ShanghaiTech University, Shanghai 201210, China; ③School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China
  • Received:2020-10-01 Online:2021-02-25 Published:2021-02-25

Abstract: G protein-coupled receptor (GPCR) family is the largest and most diverse group of membrane receptors in eukaryotes. By mediating a wide variety of physiological functions, GPCRs are important drug targets with around 500 marketed drugs. The breakthrough of GPCR structural studies leads to the determinations of over 400 structures, which highlights the diversified ligandbinding modes and signal transduction mechanisms across GPCRs. In recent years, a common activation mechanism of class A GPCRs has been discovered, by using residue-residue contact score (RRCS) that can quantitatively describes the rearrangements of residue contacts upon receptor activation. Here, we briefly summarize the approaches utilized in GPCR activation mechanism, and also discuss the significance of understanding GPCR activation mechanism on functional studies and drug discovery. 

Key words: G protein-coupled receptor, activation mechanism, allostery, drug discovery