University of Leicester
Browse

Employing novel animal models in the design of clinically efficacious GPCR ligands

Download (1.05 MB)
journal contribution
posted on 2016-02-24, 11:54 authored by S. J. Bradley, S. A. Riaz, Andrew B Tobin
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.

History

Citation

Current Opinion in Cell Biology , 2014, 27, pp. 117-125

Author affiliation

/Organisation/COLLEGE OF MEDICINE, BIOLOGICAL SCIENCES AND PSYCHOLOGY/MBSP Non-Medical Departments/Molecular & Cell Biology

Version

  • VoR (Version of Record)

Published in

Current Opinion in Cell Biology

Publisher

Elsevier for Current Opinion

issn

0955-0674

eissn

1879-0410

Copyright date

2013

Available date

2016-02-24

Publisher version

http://www.sciencedirect.com/science/article/pii/S0955067413001890

Language

en

Usage metrics

    University of Leicester Publications

    Categories

    No categories selected

    Exports

    RefWorks
    BibTeX
    Ref. manager
    Endnote
    DataCite
    NLM
    DC