A small molecule ubiquitination inhibitor blocks NF-kappa B-dependent cytokine expression in cells and rats.

@article{Swinney2002ASM,
  title={A small molecule ubiquitination inhibitor blocks NF-kappa B-dependent cytokine expression in cells and rats.},
  author={David C. Swinney and Yi-Zheng Xu and Liliana E Scarafia and Ina H Lee and Amy Y Mak and Q F Gan and Chakkodabylu S Ramesha and Mary A. Mulkins and Jim Dunn and O M So and Teresa Biegel and Marie Dinh and Pamela Volkel and Jim Barnett and Stacie A. Dalrymple and Simon D Lee and Martin Huber},
  journal={The Journal of biological chemistry},
  year={2002},
  volume={277 26},
  pages={23573-81}
}
A small molecule inhibitor of NF-kappaB-dependent cytokine expression was discovered that blocked tumor necrosis factor (TNF) alpha-induced IkappaB(alpha) degradation in MM6 cells but not the degradation of beta-catenin in Jurkat cells. Ro106-9920 blocked lipopolysaccharide (LPS)-dependent expression of TNFalpha, interleukin-1beta, and interleukin-6 in fresh human peripheral blood mononuclear cells with IC(50) values below 1 microm. Ro106-9920 also blocked TNFalpha production in a dose… CONTINUE READING

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