Next Article in Journal
Anti-Viral Drugs for Human Adenoviruses
Next Article in Special Issue
Multiple Routes to Oestrogen Antagonism
Previous Article in Journal
Cannabinoids and Reproduction: A Lasting and Intriguing History
Previous Article in Special Issue
Allosteric Inhibitors of NMDA Receptor Functions
Pharmaceuticals 2010, 3(10), 3324-3342; doi:10.3390/ph3103324
Review

Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands

 and *
Received: 9 August 2010; in revised form: 17 October 2010 / Accepted: 25 October 2010 / Published: 25 October 2010
(This article belongs to the Special Issue Allosteric Modulation)
View Full-Text   |   Download PDF [1294 KB, uploaded 25 October 2010]   |   Browse Figures
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.
Keywords: rhodopsin; metabotropic glutamate receptors; allosteric network; communication; membrane proteins rhodopsin; metabotropic glutamate receptors; allosteric network; communication; membrane proteins
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Export to BibTeX |
EndNote


MDPI and ACS Style

Yanamala, N.; Klein-Seetharaman, J. Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands. Pharmaceuticals 2010, 3, 3324-3342.

AMA Style

Yanamala N, Klein-Seetharaman J. Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands. Pharmaceuticals. 2010; 3(10):3324-3342.

Chicago/Turabian Style

Yanamala, Naveena; Klein-Seetharaman, Judith. 2010. "Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands." Pharmaceuticals 3, no. 10: 3324-3342.


Pharmaceuticals EISSN 1424-8247 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert