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1. Design and synthesis of sulfamoyl benzoic acid analogues with subnanomolar agonist activity specific to the LPA2 receptor.

Author

Patil R, Fells JI, Szabó E, Lim KG, Norman DD, Balogh A, Patil S, Strobos J, Miller DD, and Tigyi GJ

Subjects
Binding Sites, Chemistry Techniques, Synthetic, Drug Design, Drug Evaluation, Preclinical methods, Humans, Molecular Docking Simulation, Receptors, Lysophosphatidic Acid chemistry, Receptors, Lysophosphatidic Acid metabolism, Structure-Activity Relationship, Benzoates chemistry, Receptors, Lysophosphatidic Acid agonists
Abstract

Lysophosphatidic acid (LPA) is a growth factor-like mediator and a ligand for multiple GPCR. The LPA2 GPCR mediates antiapoptotic and mucosal barrier-protective effects in the gut. We synthesized sulfamoyl benzoic acid (SBA) analogues that are the first specific agonists of LPA2, some with subnanomolar activity. We developed an experimental SAR that is supported and rationalized by computational docking analysis of the SBA compounds into the LPA2 ligand-binding pocket.

Published
2014
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