Common activation mechanism of class A GPCRs
ShanghaiTech University · Chinese Academy of Sciences · +7 more institutions
Abstract
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human physiology. Understanding receptor activation mechanism is critical for discovering novel therapeutics since about one-third of all marketed drugs target members of this family. GPCR activation is an allosteric process that couples agonist binding to G-protein recruitment, with the hallmark outward movement of transmembrane helix 6 (TM6). However, what leads to TM6 movement and the key residue level changes of this movement remain less well understood. Here, we report a framework to quantify conformational changes. By analyzing the conformational changes in 234 structures from 45 class A GPCRs, we discovered a common GPCR…
Citation impact
- FWCI
- 20.08
- Percentile
- 100%
- References
- 217
Authors
16- QZQingtong ZhouCorresponding
ShanghaiTech University
- DYDehua Yang
Chinese Academy of Sciences, Shanghai Institute of Materia Medica, National Center for Drug Screening, University of Chinese Academy of Sciences
- MWMeng Wu
ShanghaiTech University, University of Chinese Academy of Sciences
- YGYu Guo
ShanghaiTech University, University of Chinese Academy of Sciences
- WGWanjing Guo
Chinese Academy of Sciences, Shanghai Institute of Materia Medica, National Center for Drug Screening, University of Chinese Academy of Sciences
Topics & keywords
- G protein-coupled receptor
- Allosteric regulation
- Signal transduction
- G protein
- Transmembrane domain
- Biology
- Binding site
- Cell biology