Inhibition of NF-kappa B activation through targeting I kappa B kinase by celastrol, a quinone methide triterpenoid.

@article{Lee2006InhibitionON,
  title={Inhibition of NF-kappa B activation through targeting I kappa B kinase by celastrol, a quinone methide triterpenoid.},
  author={J S Lee and Tae Hyeon Koo and Hyunkyung Yoon and Haeng Sun Jung and Hui Zi Jin and Kyeong Sook Lee and Young-Soo Hong and Jung Joon Lee},
  journal={Biochemical pharmacology},
  year={2006},
  volume={72 10},
  pages={1311-21}
}
Celastrol, a quinone methide triterpenoid, was isolated as an inhibitor of NF-kappaB from Celastrus orbiculatus. This compound dose-dependently inhibited a variety of stimuli-induced NF-kappa B-regulated gene expression and the DNA-binding of NF-kappa B in different cell lines without affecting DNA-binding activity of AP-1. Preincubation of celastrol completely blocked the LPS-, TNF-alpha-, or PMA-induced degradation and phosphorylation of I kappa B alpha. Importantly, celastrol inhibited IKK… CONTINUE READING

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