Allosteric modulation of g protein coupled receptors by cytoplasmic, transmembrane and extracellular ligands

Naveena Yanamala, Judith Klein-Seetharaman

Research output: Contribution to journalReview articlepeer-review

11 Scopus citations

Abstract

G protein coupled receptors (GPCRs) bind diverse classes of ligands, and depending on the receptor, these may bind in their transmembrane or the extracellular domains, demonstrating the principal ability of GPCRs to bind ligand in either domains. Most recently, it was also observed that small molecule ligands can bind in the cytoplasmic domain, and modulate binding and response to extracellular or transmembrane ligands. Thus, all three domains in GPCRs are potential sites for allosteric ligands, and whether a ligand is allosteric or orthosteric depends on the receptor. Here, we will review the evidence supporting the presence of putative binding pockets in all three domains of GPCRs and discuss possible pathways of communication between these pockets.

Original languageEnglish (US)
Pages (from-to)3324-3342
Number of pages19
JournalPharmaceuticals
Volume3
Issue number10
DOIs
StatePublished - 2010
Externally publishedYes

Keywords

  • Allosteric network
  • Communication
  • Membrane proteins
  • Metabotropic glutamate receptors
  • Rhodopsin

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science

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