Review
Nature Reviews Drug Discovery 1, 808-820 (October 2002) | doi:10.1038/nrd913
G-Protein-coupled receptor oligomerization and its potential for drug discovery
Susan R. George1,2,3, Brian F. O'Dowd1,3 & Samuel P. Lee1 About the authors
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.
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Author affiliations
- Department of Pharmacology, University of Toronto, 1 King's College Circle, Toronto, Ontario, Canada M5S 1A8.
- Department of Medicine, University of Toronto, 1 King's College Circle, Toronto, Ontario, Canada M5S 1A8.
- Centre for Addiction and Mental Health, 250 College Street, Toronto, Ontario, Canada M5T 1A8.
Correspondence to: Susan R. George1,2,3 Email: s.george@utoronto.ca
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