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.


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


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