Oligomerization of G-protein-coupled transmitter receptors.
Examples of G-protein-coupled receptors that can be biochemically detected in homo- or heteromeric complexes are emerging at an accelerated rate. Biophysical approaches have confirmed the existence of several such complexes in living cells and there is strong evidence to support the idea that dimerization is important in different aspects of receptor biogenesis and function. While the existence of G-protein-coupled-receptor homodimers raises fundamental questions about the molecular mechanisms involved in transmitter recognition and signal transduction, the formation of heterodimers raises fascinating combinatorial possibilities that could underlie an unexpected level of pharmacological diversity, and contribute to cross-talk regulation between transmission systems. Because G-protein-coupled receptors are major pharmacological targets, the existence of dimers could have important implications for the development and screening of new drugs. Here, we review the evidence supporting the existence of G-protein-coupled-receptor dimerization and discuss its functional importance.
Bouvier
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Department of Biochemistry and Groupe de Recherche sur le système Nerveux Autonome, Faculté de Médecine, Université de Montréal, P.O. Box 6128, Down-Town Station, Montréal, Quebec, H3C 3J7 Canada. Michel.Bouvier@umontreal.ca
D001692:Biological Transport; D019281:Dimerization; D004735:Energy Transfer; D005453:Fluorescence; D005816:Genetic Complementation Test; D020962:Heterotrimeric GTP-Binding Proteins / Q000378:metabolism*; D008027:Light; D018832:Molecular Chaperones / Q000378:metabolism; D011233:Precipitin Tests; D011940:Receptor Aggregation; D017447:Receptors, Dopamine D1 / Q000378:metabolism; D050641:Receptors, Dopamine D5; D011963:Receptors, GABA-A / Q000378:metabolism; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D015398:Signal Transduction
D018832:Molecular Chaperones; D017447:Receptors, Dopamine D1; D011963:Receptors, GABA-A; D017981:Receptors, Neurotransmitter; D050641:Receptors, Dopamine D5; D020962:Heterotrimeric GTP-Binding Proteins