Signal Transduction (IND 447)

G Protein Coupled Receptors

Alan V. Smrcka Ph.D.

G protein coupled receptors comprise an extensive family of cell surface receptors (over 1000 members) capable of interacting with a large diversity of stimuli to deliver information to the inside of the cell.

Structure of bacteriorhodopsin, a protein with topology similar to G protein coupled receptors.  The structure of a true G protein coupled receptor has only recently been solved (July 2000). Click on image for a larger picture.

Structure of a trimeric G protein ai (grey) b1 (red) g2 (green). Click on image for a larger picture.

GPCR's  

G proteins

References

GPCR reviews:
Ji, T.H., Grossmann, M., and Ji, I. (1998) G Protein-coupled receptors. I. Diversity of receptor-ligand interactions J. Biol. Chem. 273, 17299-17302.

G protein reviews:
Hamm, H.E. (1998) The many faces of G protein signaling. J. Biol. Chem. 267: 669-672.

RGS reviews:
Ross, E.M. and Wilkie, T.M. (2000) GTPase-Activating proteins for heterotrimeric G proteins: Regulators of G protein signaling (RGS) and RGS-like proteins. Annu. Rev. Biochem. 69:795-827.

Required Reading (Spring 2004)

Angers, S., Salahpour, A., Joly, E., Hilairet, S., Chelsky, D., Dennis, M., and Bouvier, M. (2000) Detection of b2-adrenergic receptor dimerization in living cells using bioluminescence resonance energy transfer (BRET). Proc. Natl. Acad. Sci. USA 97:3684-3689.

Berman, D.M., Wilkie, T.M., Gilman, A.G. (1996) GAIP and RGS4 are GTPase-activating proteins for the G_i subfamily of G protein a subunits. Cell 86:445-452.

Relevant Links

The following link is to an extensive database of G protein coupled receptors   GPCR database