Structural Studies of G Protein-Coupled Receptors

Mol Cells. 2015 Oct;38(10):836-42. doi: 10.14348/molcells.2015.0263. Epub 2015 Oct 15.

Abstract

G protein-coupled receptors (GPCRs) constitute the largest and the most physiologically important membrane protein family that recognizes a variety of environmental stimuli, and are drug targets in the treatment of numerous diseases. Recent progress on GPCR structural studies shed light on molecular mechanisms of GPCR ligand recognition, activation and allosteric modulation, as well as structural basis of GPCR dimerization. In this review, we will discuss the structural features of GPCRs and structural insights of different aspects of GPCR biological functions.

Keywords: GPCR; activation; allosteric modulation; ligand recognition; structure.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Allosteric Regulation
  • Amino Acid Motifs
  • Humans
  • Ligands
  • Protein Multimerization
  • Protein Structure, Tertiary
  • Receptors, G-Protein-Coupled / chemistry*
  • Receptors, G-Protein-Coupled / classification
  • Receptors, G-Protein-Coupled / physiology*

Substances

  • Ligands
  • Receptors, G-Protein-Coupled