GPR35 as a Novel Therapeutic Target
Open Access
- 1 January 2011
- journal article
- Published by Frontiers Media SA in Frontiers in Endocrinology
- Vol. 2, 68
- https://doi.org/10.3389/fendo.2011.00068
Abstract
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.Keywords
This publication has 66 references indexed in Scilit:
- G-protein coupled receptor 35 (GPR35) activation and inflammatory pain: Studies on the antinociceptive effects of kynurenic acid and zaprinastNeuropharmacology, 2011
- Tyrphostin analogs are GPR35 agonistsFEBS Letters, 2011
- Pharmacology of GPR55 in Yeast and Identification of GSK494581A as a Mixed-Activity Glycine Transporter Subtype 1 Inhibitor and GPR55 AgonistJournal of Pharmacology and Experimental Therapeutics, 2011
- RhoA/ROCK signaling is essential for multiple aspects of VEGF‐mediated angiogenesisThe FASEB Journal, 2010
- Kynurenic Acid Triggers Firm Arrest of Leukocytes to Vascular Endothelium under Flow ConditionsPublished by Elsevier BV ,2009
- Recent advances in the treatment of amyotrophic lateral sclerosis. Emphasis on kynurenine pathway inhibitors.Central Nervous System Agents in Medicinal Chemistry, 2009
- Two pathways for lysophosphatidic acid productionBiochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 2008
- β-Arrestins and Cell SignalingAnnual Review of Physiology, 2007
- Rac Regulates Endothelial Morphogenesis and Capillary AssemblyMolecular Biology of the Cell, 2002
- Altered Expression of Inhibitory Guanine Nucleotide Regulatory Proteins (Gi ) in Spontaneously Hypertensive RatsAmerican Journal of Hypertension, 1991