Biomolecules & Therapeutics  2017;25(1):4-11

doi:10.4062/biomolther.2016.169

Recent Progress in Understanding the Conformational Mechanism of Heterotrimeric G Protein Activation.

Nguyen Minh DUC 1 ; Hee Ryung KIM ; Ka Young CHUNG

Affiliations

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Keywords

G protein; G protein-coupled receptor; Structure; Dynamics

Country

Republic of Korea

Language

English

Abstract

Heterotrimeric G proteins are key intracellular coordinators that receive signals from cells through activation of cognate G protein-coupled receptors (GPCRs). The details of their atomic interactions and structural mechanisms have been described by many biochemical and biophysical studies. Specifically, a framework for understanding conformational changes in the receptor upon ligand binding and associated G protein activation was provided by description of the crystal structure of the β2-adrenoceptor-Gs complex in 2011. This review focused on recent findings in the conformational dynamics of G proteins and GPCRs during activation processes.