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GPCRs Revisited: New Insights Lead to Novel Drugs
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Expanding the Concept of G Protein-Coupled Receptor (GPCR) Dimer Asymmetry towards GPCR-Interacting Proteins

by Maud Kamal 1,2, Pascal Maurice 1,2 and Ralf Jockers 1,2,*
1
Institut Cochin, Université Paris Descartes, CNRS, Paris, France
2
Inserm, U1016, Paris, France
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2011, 4(2), 273-284; https://doi.org/10.3390/ph4020273
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)
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. View Full-Text
Keywords: GPCR; dimerization; GIP; allosterism   GPCR; dimerization; GIP; allosterism  
MDPI and ACS Style

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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