Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA(2) Receptor

[Image: see text] Lysophosphatidic acid (LPA) is a growth factor-like mediator and a ligand for multiple GPCR. The LPA(2) 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 LPA(2...

Descripción completa

Detalles Bibliográficos
Autores principales: Patil, Renukadevi, Fells, James I., Szabó, Erzsébet, Lim, Keng G., Norman, Derek D., Balogh, Andrea, Patil, Shivaputra, Strobos, Jur, Miller, Duane D., Tigyi, Gábor J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4148159/
https://www.ncbi.nlm.nih.gov/pubmed/25100502
http://dx.doi.org/10.1021/jm5007116
_version_ 1782332566777364480
author Patil, Renukadevi
Fells, James I.
Szabó, Erzsébet
Lim, Keng G.
Norman, Derek D.
Balogh, Andrea
Patil, Shivaputra
Strobos, Jur
Miller, Duane D.
Tigyi, Gábor J.
author_facet Patil, Renukadevi
Fells, James I.
Szabó, Erzsébet
Lim, Keng G.
Norman, Derek D.
Balogh, Andrea
Patil, Shivaputra
Strobos, Jur
Miller, Duane D.
Tigyi, Gábor J.
author_sort Patil, Renukadevi
collection PubMed
description [Image: see text] Lysophosphatidic acid (LPA) is a growth factor-like mediator and a ligand for multiple GPCR. The LPA(2) 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 LPA(2), some with subnanomolar activity. We developed an experimental SAR that is supported and rationalized by computational docking analysis of the SBA compounds into the LPA(2) ligand-binding pocket.
format Online
Article
Text
id pubmed-4148159
institution National Center for Biotechnology Information
language English
publishDate 2014
publisher American Chemical Society
record_format MEDLINE/PubMed
spelling pubmed-41481592015-08-06 Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA(2) Receptor Patil, Renukadevi Fells, James I. Szabó, Erzsébet Lim, Keng G. Norman, Derek D. Balogh, Andrea Patil, Shivaputra Strobos, Jur Miller, Duane D. Tigyi, Gábor J. J Med Chem [Image: see text] Lysophosphatidic acid (LPA) is a growth factor-like mediator and a ligand for multiple GPCR. The LPA(2) 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 LPA(2), some with subnanomolar activity. We developed an experimental SAR that is supported and rationalized by computational docking analysis of the SBA compounds into the LPA(2) ligand-binding pocket. American Chemical Society 2014-08-06 2014-08-28 /pmc/articles/PMC4148159/ /pubmed/25100502 http://dx.doi.org/10.1021/jm5007116 Text en Copyright © 2014 American Chemical Society Terms of Use (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html)
spellingShingle Patil, Renukadevi
Fells, James I.
Szabó, Erzsébet
Lim, Keng G.
Norman, Derek D.
Balogh, Andrea
Patil, Shivaputra
Strobos, Jur
Miller, Duane D.
Tigyi, Gábor J.
Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA(2) Receptor
title Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA(2) Receptor
title_full Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA(2) Receptor
title_fullStr Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA(2) Receptor
title_full_unstemmed Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA(2) Receptor
title_short Design and Synthesis of Sulfamoyl Benzoic Acid Analogues with Subnanomolar Agonist Activity Specific to the LPA(2) Receptor
title_sort design and synthesis of sulfamoyl benzoic acid analogues with subnanomolar agonist activity specific to the lpa(2) receptor
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4148159/
https://www.ncbi.nlm.nih.gov/pubmed/25100502
http://dx.doi.org/10.1021/jm5007116
work_keys_str_mv AT patilrenukadevi designandsynthesisofsulfamoylbenzoicacidanalogueswithsubnanomolaragonistactivityspecifictothelpa2receptor
AT fellsjamesi designandsynthesisofsulfamoylbenzoicacidanalogueswithsubnanomolaragonistactivityspecifictothelpa2receptor
AT szaboerzsebet designandsynthesisofsulfamoylbenzoicacidanalogueswithsubnanomolaragonistactivityspecifictothelpa2receptor
AT limkengg designandsynthesisofsulfamoylbenzoicacidanalogueswithsubnanomolaragonistactivityspecifictothelpa2receptor
AT normanderekd designandsynthesisofsulfamoylbenzoicacidanalogueswithsubnanomolaragonistactivityspecifictothelpa2receptor
AT baloghandrea designandsynthesisofsulfamoylbenzoicacidanalogueswithsubnanomolaragonistactivityspecifictothelpa2receptor
AT patilshivaputra designandsynthesisofsulfamoylbenzoicacidanalogueswithsubnanomolaragonistactivityspecifictothelpa2receptor
AT strobosjur designandsynthesisofsulfamoylbenzoicacidanalogueswithsubnanomolaragonistactivityspecifictothelpa2receptor
AT millerduaned designandsynthesisofsulfamoylbenzoicacidanalogueswithsubnanomolaragonistactivityspecifictothelpa2receptor
AT tigyigaborj designandsynthesisofsulfamoylbenzoicacidanalogueswithsubnanomolaragonistactivityspecifictothelpa2receptor

Ejemplares similares