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Pharmaceuticals 2011, 4(2), 244-272; doi:10.3390/ph4020244
Review

GPCRs Revisited: New Insights Lead to Novel Drugs

1,*  and 2
Received: 6 December 2010; in revised form: 22 December 2010 / Accepted: 18 January 2011 / Published: 25 January 2011
(This article belongs to the Special Issue GPCR Based Drug Discovery)
View Full-Text   |   Download PDF [216 KB, uploaded 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 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

AMA Style

Eglen RM, Reisine T. GPCRs Revisited: New Insights Lead to Novel Drugs. Pharmaceuticals. 2011; 4(2):244-272.

Chicago/Turabian Style

Eglen, Richard M.; Reisine, Terry. 2011. "GPCRs Revisited: New Insights Lead to Novel Drugs." Pharmaceuticals 4, no. 2: 244-272.



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