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Pharmaceuticals 2011, 4(2), 244-272;

GPCRs Revisited: New Insights Lead to Novel Drugs

Bio-Discovery, PerkinElmer Life and Analytical Sciences, 940 Winter St., Waltham, MA 02451, USA
Reisine Biotechnology Consultants, 10327 Rossbury Place, Los Angeles, CA 90064, USA
Author to whom correspondence should be addressed.
Received: 6 December 2010 / Revised: 22 December 2010 / Accepted: 18 January 2011 / Published: 25 January 2011
(This article belongs to the Special Issue GPCR Based Drug Discovery)
Full-Text   |   PDF [216 KB, uploaded 25 January 2011]


GPCRs play a critical role in human physiology and are a prime target for drug discovery globally. Novel insights into the functions of GPCRs are providing unique approaches to modulate these proteins to generate unique drug candidates. Next generation ligands include those with novel pharmacologies such as allosteric regulators as well pepducins, that affect the interaction of GPCRs with G proteins, to either block selective receptor signaling pathways or mimic the actions of intracellular domains of receptors, thereby activating GPCRs to signal selectively to intracellular pathways. We will review these new concepts and then discuss how they may be exploited using modern discovery technologies to provide novel drug candidates for the future. View Full-Text
Keywords: GPCR; G protein; allosterism; dualsteric; oligomerization; pharmacophore; crystal structure; NMR; DMR; pepducin GPCR; G protein; allosterism; dualsteric; oligomerization; pharmacophore; crystal structure; NMR; DMR; pepducin
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Eglen, R.M.; Reisine, T. GPCRs Revisited: New Insights Lead to Novel Drugs. Pharmaceuticals 2011, 4, 244-272.

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