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

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

Research output: Contribution to journalArticle

8 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)7136-7140
Number of pages5
JournalJournal of Medicinal Chemistry
Volume57
Issue number16
DOIs
StatePublished - Jan 1 2014

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Lysophosphatidic Acid Receptors
Benzoic Acid
Ligands
Intercellular Signaling Peptides and Proteins

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

Cite this

Design and synthesis of sulfamoyl benzoic acid analogues with subnanomolar agonist activity specific to the LPA2 receptor. / Patil, Renukadevi; Fells, James I.; Szabó, Erzsébet; Lim, Keng G.; Norman, Derek D.; Balogh, Andrea; Patil, Shivaputra; Strobos, Jur; Miller, Duane; Tigyi, Gabor.

In: Journal of Medicinal Chemistry, Vol. 57, No. 16, 01.01.2014, p. 7136-7140.

Research output: Contribution to journalArticle

Patil, Renukadevi ; Fells, James I. ; Szabó, Erzsébet ; Lim, Keng G. ; Norman, Derek D. ; Balogh, Andrea ; Patil, Shivaputra ; Strobos, Jur ; Miller, Duane ; Tigyi, Gabor. / Design and synthesis of sulfamoyl benzoic acid analogues with subnanomolar agonist activity specific to the LPA2 receptor. In: Journal of Medicinal Chemistry. 2014 ; Vol. 57, No. 16. pp. 7136-7140.
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AU - Lim, Keng G.

AU - Norman, Derek D.

AU - Balogh, Andrea

AU - Patil, Shivaputra

AU - Strobos, Jur

AU - Miller, Duane

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