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Nat Rev Drug Discov. 2002 Oct;1(10):808-20.

G-protein-coupled receptor oligomerization and its potential for drug discovery.

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Department of Pharmacology, University of Toronto, 1 King's College Circle, Toronto, Ontario, Canada M5S 1A8.


G-protein-coupled receptors (GPCRs) represent by far the largest class of targets for modern drugs. Virtually all therapeutics that are directed towards GPCRs have been designed using assays that presume that these receptors are monomeric. The recent realization that these receptors form homo-oligomeric and hetero-oligomeric complexes has added a new dimension to rational drug design. However, this important aspect of GPCR biology remains largely unincorporated into schemes to search for new therapeutics. This review provides a synopsis of the current thinking surrounding GPCR homo-oligomerization and hetero-oligomerization and shows how new models point towards unexplored avenues in the development of new therapies.

[Indexed for MEDLINE]

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