GPR35 as a novel therapeutic target

Mackenzie, A.E., Lappin, J.E., Taylor, D.L., Nicklin, S.A. and Milligan, G. (2011) GPR35 as a novel therapeutic target. Frontiers in Endocrinology, 2, 68. (doi: 10.3389/fendo.2011.00068) (PMID:22654822) (PMCID:PMC3356001)

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G protein-coupled receptors (GPCRs) remain the best studied class of cell surface receptors and the most tractable family of proteins for novel small molecule drug discovery. Despite this, a considerable number of GPCRs remain poorly characterized and in a significant number of cases, endogenous ligand(s) that activate them remain undefined or are of questionable physiological relevance. GPR35 was initially discovered over a decade ago but has remained an “orphan” receptor. Recent publications have highlighted novel ligands, both endogenously produced and synthetic, which demonstrate significant potency at this receptor. Furthermore, evidence is accumulating which highlights potential roles for GPR35 in disease and therefore, efforts to characterize GPR35 more fully and develop it as a novel therapeutic target in conditions that range from diabetes and hypertension to asthma are increasing. Recently identified ligands have shown marked species selective properties, indicating major challenges for future drug development. As we begin to understand these issues, the continuing efforts to identify novel agonist and antagonist ligands for GPR35 will help to decipher its true physiological relevance; translating multiple assay systems in vitro, to animal disease systems in vivo and finally to man.

Item Type:Articles
Glasgow Author(s) Enlighten ID:Nicklin, Professor Stuart and Milligan, Professor Graeme and Mackenzie, Miss Amanda
Authors: Mackenzie, A.E., Lappin, J.E., Taylor, D.L., Nicklin, S.A., and Milligan, G.
College/School:College of Medical Veterinary and Life Sciences > Institute of Cardiovascular and Medical Sciences
College of Medical Veterinary and Life Sciences > Institute of Molecular Cell and Systems Biology
Journal Name:Frontiers in Endocrinology
Publisher:Frontiers Research Foundation
ISSN (Online):1664-2392
Copyright Holders:Copyright © 2016 The Authors
First Published:First published in Frontiers in Endocrinology 2:68
Publisher Policy:Reproduced in accordance with the copyright policy of the publisher

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