2. Academic Validation
  3. Design and synthesis of sulfamoyl benzoic acid analogues with subnanomolar agonist activity specific to the LPA2 receptor

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

  • J Med Chem. 2014 Aug 28;57(16):7136-40. doi: 10.1021/jm5007116.
Renukadevi Patil 1,  James I Fells,  Erzsébet Szabó,  Keng G Lim,  Derek D Norman,  Andrea Balogh,  Shivaputra Patil,  Jur Strobos,  Duane D Miller,  Gábor J Tigyi
Affiliations

Affiliation

  • 1 Departments of Pharmaceutical Sciences and ‡Physiology, The University of Tennessee Health Science Center , Memphis, Tennessee 894 Union Avenue 38163 United States.
PMID: 25100502 DOI: 10.1021/jm5007116
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.

Figures