G-Protein-coupled receptor oligomerization and its potential for drug discovery
Top Cited Papers
- 1 October 2002
- journal article
- review article
- Published by Springer Nature in Nature Reviews Drug Discovery
- Vol. 1 (10) , 808-820
- https://doi.org/10.1038/nrd913
Abstract
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.Keywords
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