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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