Broad-spectrum amino acid-sensing class C G-protein coupled receptors: molecular mechanisms, physiological significance and options for drug development

Arthur D Conigrave; David R Hampson

doi:10.1016/j.pharmthera.2010.04.007

Broad-spectrum amino acid-sensing class C G-protein coupled receptors: molecular mechanisms, physiological significance and options for drug development

Pharmacol Ther. 2010 Sep;127(3):252-60. doi: 10.1016/j.pharmthera.2010.04.007. Epub 2010 May 6.

Authors

Arthur D Conigrave¹, David R Hampson

Affiliation

¹ School of Molecular Bioscience (G08), University of Sydney, NSW 2006, Australia. a.conigrave@usyd.edu.au

PMID: 20451554
DOI: 10.1016/j.pharmthera.2010.04.007

Abstract

In this article, we consider the molecular mechanisms that underlie broad-spectrum amino acid sensing by a discrete subgroup of class C G-protein-coupled receptors that includes the calcium-sensing receptor, GPRC6A and heterodimers composed of two closely related receptor subunits, T1R(1) and T1R(3). We consider their physiological significance highlighting their diverse spectrum of cellular responses and the phenotypes of global and conditional knock-out mice. In addition, we consider strategies for the development of new drugs that target these receptors.

Publication types

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

MeSH terms

Amino Acids / metabolism*
Animals
Dimerization
Drug Design*
Humans
Ligands
Mice
Mice, Knockout
Models, Molecular
Protein Binding
Receptors, Amino Acid / metabolism
Receptors, Amino Acid / physiology
Receptors, G-Protein-Coupled / chemistry
Receptors, G-Protein-Coupled / genetics
Receptors, G-Protein-Coupled / metabolism
Receptors, G-Protein-Coupled / physiology*
Signal Transduction

Substances

Amino Acids
GPRC6A protein, human
GPRC6A protein, mouse
Ligands
Receptors, Amino Acid
Receptors, G-Protein-Coupled
taste receptors, type 1