2. Academic Validation
  3. Novel IKK inhibitors: beta-carbolines

Novel IKK inhibitors: beta-carbolines

  • Bioorg Med Chem Lett. 2003 Jul 21;13(14):2419-22. doi: 10.1016/s0960-894x(03)00408-6.
Alfredo C Castro 1,  Luan C Dang,  François Soucy,  Louis Grenier,  Hormoz Mazdiyasni,  Maria Hottelet,  Lana Parent,  Christine Pien,  Vito Palombella,  Julian Adams
Affiliations

Affiliation

  • 1 Millennium Pharmaceuticals Inc., 35 Landsdowne Street, 02139, Cambridge, MA, USA.
PMID: 12824047 DOI: 10.1016/s0960-894x(03)00408-6
Abstract

Inhibitors of IkappaB kinase (IKK) have long been sought as specific regulators of NF-kappaB. A screening effort of the endogenous IKK complex allowed us to identify 5-bromo-6-methoxy-beta-carboline as a nonspecific IKK Inhibitor. Optimization of this beta-carboline natural product derivative resulted in a novel class of selective IKK inhibitors with IC(50)s in the nanomolar range. In addition, we show that one of these beta-carboline analogues inhibits the phosphorylation of IkappaBalpha and subsequent activation of NF-kappaB in whole cells, as well as blocking TNF-alpha release in LPS-challenged mice.

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