Document Detail

Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation.
MedLine Citation:
PMID:  22003428     Owner:  NLM     Status:  Publisher    
NOD1 (nucleotide-binding oligomerization domain 1) protein is a member of the NLR (NACHT and leucine rich repeat domain containing proteins) protein family, which plays a key role in innate immunity as a sensor of specific microbial components derived from bacterial peptidoglycans and induction of inflammatory responses. Mutations in NOD proteins have been associated with various inflammatory diseases that affect NF-κB (nuclear factor κB) activity, a major signaling pathway involved in apoptosis, inflammation, and immune response. A luciferase-based reporter gene assay was utilized in a high-throughput screening program conducted under the NIH-sponsored Molecular Libraries Probe Production Center Network program to identify the active scaffolds. Herein, we report the chemical synthesis, structure-activity relationship studies, downstream counterscreens, secondary assay data, and pharmacological profiling of the 2-aminobenzimidazole lead (compound 1c, ML130) as a potent and selective inhibitor of NOD1-induced NF-κB activation.
Pasha M Khan; Ricardo G Correa; Daniela B Divlianska; Satyamaheshwar Peddibhotla; E Hampton Sessions; Gavin Magnuson; Brock Brown; Eigo Suyama; Hongbin Yuan; Arianna Mangravita-Novo; Michael Vicchiarelli; Ying Su; Stefan Vasile; Layton H Smith; Paul W Diaz; John C Reed; Gregory P Roth
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-8-05
Journal Detail:
Title:  ACS medicinal chemistry letters     Volume:  2     ISSN:  1948-5875     ISO Abbreviation:  -     Publication Date:  2011 Oct 
Date Detail:
Created Date:  2011-10-17     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101521073     Medline TA:  ACS Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  780-785     Citation Subset:  -    
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