Operational models of allosteric modulation of G protein-coupled receptors
10.16438/j.0513-4870.2016-0775
- VernacularTitle:G蛋白偶联受体变构调节的应用模型
- Author:
Hao GONG
1
;
Shuo ZHANG
1
;
Richard Dequan YE
1
Author Information
1. School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China
- Publication Type:REVIEWS
- Keywords:
G protein-coupled receptor;
allosteric regulation;
allosteric site;
ternary complex model
- From:
Acta Pharmaceutica Sinica
2016;51(12):1829-
- CountryChina
- Language:Chinese
-
Abstract:
Since the Monod-Wyman-Changeux (MWC) model was initially proposed to explain the allosteric interactions between proteins and their ligands 50 years ago, there have been various models and hypotheses such as the induced-fit model on the interaction. These theoretical developments have been used broadly in the study of allosteric modulations of enzymes and receptors. In 1980, Lefkowitz and coworkers proposed a ternary complex model (TCM) for the regulatory mechanism of G protein-coupled receptors (GPCRs) that laid the theoretical foundation in the study of allosteric sites and ligands of GPCRs, the largest family of known receptors. The findings on how ligands interact with receptors to cause a functional response have significantly impacted the drug discovery field and accelerated the identification of allosteric modulators.
