Work

Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA2 Receptor

Year: 2014

Type: article

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.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/jm5007116

Authors: Renukadevi Patil, James I. Fells, Erzsébet Szabó, Keng G. Lim, Derek D. Norman, Andrea Balogh, Shivaputra Patil, Jur Strobos, Duane D. Miller, Gábor J. Tigyi

Institutions: University of Tennessee Health Science Center, RxBio (United States)

Language: English

Topic: Sphingolipid Metabolism and Signaling

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,500

Funders: American Cancer Society, U.S. Department of Veterans Affairs, National Institute of Allergy and Infectious Diseases

Awards: Analysis of Radiomitigative Cell Signaling, G1522443849, G2216863125, IND-Enabling Preclinical Development of a New Radiomitigator, G9000113063

OpenAlex ID: W2374725955

FWCI: 0.682

Cites: 14

Cited by: 15

Related to: 10