Document Detail


Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation.
MedLine Citation:
PMID:  22003428     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
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
Related Documents :
24287118 - Ghrelin protects human umbilical vein endothelial cells against high glucose-induced ap...
23959098 - Anti-apoptotic phenotypes of cholestan-3β,5α,6β-triol-resistant human cholangiocytes...
24025398 - Expanding role of delta-like 4 mediated notch signaling in cardiovascular and metabolic...
23046548 - Opsonization of malaria-infected erythrocytes activates the inflammasome and enhances i...
15551798 - Comparison of two different protocols for the induction of maturation of human dendriti...
12530648 - 11beta-hydroxysteroid dehydrogenase type 1 in differentiating omental human preadipocyt...
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:  -    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  The good behavior game and the future of prevention and treatment.
Next Document:  Site-Specific Spectroscopic Reporters of the Local Electric Field, Hydration, Structure, and Dynamic...