Article,

Coupling mode of receptors and G proteins

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Naunyn Schmiedebergs Arch Pharmacol, 379 (5): 435-43 (May 2009)Hein, Peter Bunemann, Moritz Research Support, Non-U.S. Gov't Review Germany Naunyn-Schmiedeberg's archives of pharmacology Naunyn Schmiedebergs Arch Pharmacol. 2009 May;379(5):435-43. Epub 2008 Dec 2..

Abstract

Signaling via G-protein-coupled receptors (GPCRs) is crucial to many physiological and pathophysiological processes in multicellular organisms, and GPCRs themselves are targets for important drugs. Classical cell supplementation experiments suggest a collision coupling model, in which receptors and G proteins diffuse randomly within the cell membrane and interact only if receptors are activated. This model is also backed by kinetic and live cell imaging data. According to the challenging theory, receptors and G proteins are precoupled--meaning they are forming stable complexes in the absence of agonist, which prevail during signaling. This model has been favored on the basis of copurification and coimmunoprecipitation of inactive receptors with G proteins and more recently by some approaches measuring energy transfer between labeled receptors and G proteins. This article reviews key findings regarding the receptor/G protein coupling mode, including most recent findings obtained by optical techniques.

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