Toxicol Res.  2013 Sep;29(3):149-155.

Structural Aspects of GPCR-G Protein Coupling

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

Abstract

G protein-coupled receptors (GPCRs) are membrane receptors; approximately 40% of drugs on the market target GPCRs. A precise understanding of the activation mechanism of GPCRs would facilitate the development of more effective and less toxic drugs. Heterotrimeric G proteins are important molecular switches in GPCR-mediated signal transduction. An agonist-activated receptor interacts with specific sites on G proteins and promotes the release of GDP from the Galpha subunit. Because of the important biological role of the GPCR-G protein coupling, conformational changes in the G protein upon receptor coupling have been of great interest. One of the most important questions was the interface between the GPCR and G proteins and the structural mechanism of GPCR-induced G protein activation. A number of biochemical and biophysical studies have been performed since the late 80s to address these questions; there was a significant breakthrough in 2011 when the crystal structure of a GPCR-G protein complex was solved. This review discusses the structural aspects of GPCR-G protein coupling by comparing the results of previous biochemical and biophysical studies to the GPCR-G protein crystal structure.

Keyword

GPCR; G protein; Structure

MeSH Terms

GTP-Binding Proteins
Guanosine Diphosphate
Heterotrimeric GTP-Binding Proteins
Membranes
Signal Transduction
GTP-Binding Proteins
Guanosine Diphosphate
Heterotrimeric GTP-Binding Proteins
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