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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; in revised form: 22 December 2010 / Accepted: 18 January 2011 / Published: 25 January 2011
Abstract: 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.
Keywords: GPCR; G protein; allosterism; dualsteric; oligomerization; pharmacophore; crystal structure; NMR; DMR; pepducin
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MDPI and ACS Style
Eglen, R.M.; Reisine, T. GPCRs Revisited: New Insights Lead to Novel Drugs. Pharmaceuticals 2011, 4, 244-272.
Eglen RM, Reisine T. GPCRs Revisited: New Insights Lead to Novel Drugs. Pharmaceuticals. 2011; 4(2):244-272.
Eglen, Richard M.; Reisine, Terry. 2011. "GPCRs Revisited: New Insights Lead to Novel Drugs." Pharmaceuticals 4, no. 2: 244-272.