2. Academic Validation
  3. Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activation pathway

Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activation pathway

  • Bioorg Med Chem. 2010 Mar 1;18(5):1918-24. doi: 10.1016/j.bmc.2010.01.039.
Karl J Okolotowicz 1,  Ranxin Shi,  Xueying Zheng,  Mary MacDonald,  John C Reed,  John R Cashman
Affiliations

Affiliation

  • 1 Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA. kokolotowicz@hbri.org
PMID: 20153655 DOI: 10.1016/j.bmc.2010.01.039
Abstract

Dysregulated antigen receptor-mediated NF-kappaB activation can contribute to development of autoimmunity, chronic inflammation, and malignancy. A chemical biology screening strategy has identified a substituted benzimidazole that selectively inhibits antigen receptor-mediated NF-kappaB activation without blocking Other NF-kappaB activation pathways. A library of analogs was synthesized and the structure-activity relationship and metabolic stability for the series is presented.

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