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Title: Employing novel animal models in the design of clinically efficacious GPCR ligands
Authors: Bradley, S. J.
Riaz, S. A.
Tobin, Andrew B
First Published: 31-Dec-2013
Publisher: Elsevier for Current Opinion
Citation: Current Opinion in Cell Biology , 2014, 27, pp. 117-125
Abstract: The headline success of targeting GPCRs in human diseases has masked the fact that many GPCR drug discovery programmes fail. This is despite a substantial increase in our understanding of GPCR pharmacology that has provided an array of ligands that target both orthosteric and allosteric sites as well as ligands that show stimulus bias. From this plethora of pharmacological possibilities, can we design ligand properties that would deliver maximal clinical efficacy with lowest toxicity? This may be achieved through animal models that both validate a particular GPCR as a target as well as revealing the signalling mechanisms that underlie receptor-mediated physiological and clinical responses. In this article, we examine recent novel transgenic models being employed to address this issue.
DOI Link: 10.1016/
ISSN: 0955-0674
eISSN: 1879-0410
Version: Publisher Version
Status: Peer-reviewed
Type: Journal Article
Rights: Copyright © 2013 The Authors. Published by Elsevier Ltd. Open access under CC BY-NC-ND license ( ) .
Appears in Collections:Published Articles, College of Medicine, Biological Sciences and Psychology

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