| Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation. | |
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MedLine Citation:
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PMID: 22003428 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: JOURNAL ARTICLE Date: 2011-8-05 |
Journal Detail:
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Title: ACS medicinal chemistry letters Volume: 2 ISSN: 1948-5875 ISO Abbreviation: - Publication Date: 2011 Oct |
Date Detail:
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Created Date: 2011-10-17 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101521073 Medline TA: ACS Med Chem Lett Country: - |
Other Details:
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Languages: ENG Pagination: 780-785 Citation Subset: - |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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