Biomol Ther.  2017 Jan;25(1):4-11. 10.4062/biomolther.2016.169.

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

Affiliations
  • 1School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea. kychung2@skku.edu

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.

Keyword

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

MeSH Terms

GTP-Binding Proteins*
Heterotrimeric GTP-Binding Proteins
GTP-Binding Proteins
Heterotrimeric GTP-Binding Proteins
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