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G-protein coupled receptors

G-protein coupled receptors (GPCR) are the largest superfamily of cell surface receptors and indeed of all protein families. Their signature motif are seven helices, that transverse the membrane (Figure below), dividing the proteins into cytoplasmic, transmembrane and extracellular domains. The function of GPCR is to transduce signals that induce a cellular response to the environment. The GPCR family has great pharmacological importance, as demonstrated by the fact that 50-60% of approved drugs elicit their therapeutic effect by selectively addressing members of the GPCR family (Muller, G. (2000) Towards 3D structures of G protein-coupled receptors: a multidisciplinary approach. Curr. Med. Chem. 7(9), 861-888, Gudermann, T., B. Nurnberg, and G. Schultz, Receptors and G proteins as primary components of transmembrane signal transduction. Part 1. G-protein-coupled receptors: structure and function. J Mol Med, 1995. 73(2): p. 51-63; Drews, J., Genomic sciences and the medicine of tomorrow. Nat Biotechnol, 1996. 14(11): p. 1516-8). This website is designed to provide an overview about current molecular level knowledge on the structure, function and dynamics of this important protein family. For copyright reasons all links to original publications are password protected, but the references are given.

Figure: Signature of GPCR: 7 transmembrane helices divide the protein into three domains, the cytoplasmic, the transmembrane and the extracellular domains.



Receptor activation

Receptor phosphorylation

Receptor modeling

Receptor dynamics

Protein-protein interactions

Receptor folding

Receptor expression and purification

Receptor functions

Homology between subfamilies

Generic GPCR numbering system

G-protein coupled receptor web resources

Receptor Chimera

Ligand Binding


2002 Judith Klein-Seetharaman, University of Pittsburgh. This website was created December 3, 2002 and updated January 6, 2003. For questions or comments please contact Judith Klein-Seetharaman at