Design of next-generation G protein–coupled receptor drugs: linking novel pharmacology and in vivo animal models

Bradley, S. J. and Tobin, A. B. (2016) Design of next-generation G protein–coupled receptor drugs: linking novel pharmacology and in vivo animal models. Annual Review of Pharmacology and Toxicology, 56(1), pp. 535-559. (doi: 10.1146/annurev-pharmtox-011613-140012) (PMID:26738479)

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Abstract

Despite the fact that G protein-coupled receptors (GPCRs) are the most successful drug targets in history, this supergene family of cell surface receptors has yet to be fully exploited as targets in the treatment of human disease. Here, we present optimism that this may change in the future by reviewing the substantial progress made in the understanding of GPCR molecular pharmacology that has generated an extensive toolbox of ligand types that include orthosteric, allosteric, and bitopic ligands, many of which show signaling bias. We discuss how combining these advances with recently described transgenic, chemical genetic, and optogenetic animal models will provide the framework to allow for the rational design of next-generation GPCR drugs that possess increased therapeutic efficacy and decreased adverse/toxic responses.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Tobin, Andrew and Bradley, Dr Sophie
Authors: Bradley, S. J., and Tobin, A. B.
College/School:College of Medical Veterinary and Life Sciences > Institute of Molecular Cell and Systems Biology
Research Group:Pharmacology and Pharmacy Toxicology
Journal Name:Annual Review of Pharmacology and Toxicology
Publisher:Annual Reviews
ISSN:0362-1642
ISSN (Online):1545-4304

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