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Pharmaceuticals 2011, 4(2), 273-284; doi:10.3390/ph4020273

Expanding the Concept of G Protein-Coupled Receptor (GPCR) Dimer Asymmetry towards GPCR-Interacting Proteins

Institut Cochin, Université Paris Descartes, CNRS, Paris, France
Inserm, U1016, Paris, France
Author to whom correspondence should be addressed.
Received: 6 December 2010 / Revised: 7 January 2011 / Accepted: 14 January 2011 / Published: 25 January 2011
(This article belongs to the Special Issue GPCR Based Drug Discovery)
View Full-Text   |   Download PDF [289 KB, uploaded 25 January 2011]   |  


G protein-coupled receptors (GPCRs), major targets of drug discovery, are organized in dimeric and/or oligomeric clusters. The minimal oligomeric unit, the dimer, is composed of two protomers, which can behave differently within the dimer. Several examples of GPCR asymmetry within dimers at the level of ligand binding, ligand-promoted conformational changes, conformational changes within transmembrane domains, G protein coupling, and most recently GPCR-interacting proteins (GIPs), have been reported in the literature. Asymmetric organization of GPCR dimers has important implications on GPCR function and drug design. Indeed, the extension of the “asymmetry concept” to GIPs adds a new level of specific therapeutic intervention.
Keywords: GPCR; dimerization; GIP; allosterism   GPCR; dimerization; GIP; allosterism  
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Kamal, M.; Maurice, P.; Jockers, R. Expanding the Concept of G Protein-Coupled Receptor (GPCR) Dimer Asymmetry towards GPCR-Interacting Proteins. Pharmaceuticals 2011, 4, 273-284.

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