Document Detail

Design and Synthesis of Sulfamoyl Benzoic Acid Analogs with Subnanomolar Agonist Activity Specific to the LPA2 Receptor.
MedLine Citation:
PMID:  25100502     Owner:  NLM     Status:  Publisher    
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) analogs that are the first specific agonists of LPA2, some with subnanomolar activity. We also developed an experimental SAR that is supported and rationalized by computational docking analysis of the SBA compounds into the LPA2 ligand-binding pocket.
Renukadevi Patil; James I Fells; Erzsebet Szabo; Keng Gatt Lim; Derek Norman; Andrea Balogh; Shivaputra Appanna Patil; Jur Strobos; Duane D Miller; Gabor Tigyi
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-8-6
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2014 Aug 
Date Detail:
Created Date:  2014-8-7     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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