MX1013, a dipeptide caspase inhibitor with potent in vivo antiapoptotic activity

  title={MX1013, a dipeptide caspase inhibitor with potent in vivo antiapoptotic activity},
  author={W. Yang and J. Guastella and J. Huang and Y. Wang and L. Zhang and Dong Xue and M. Tran and R. Woodward and S. Kasibhatla and B. Tseng and J. Drewe and S. Cai},
  journal={British Journal of Pharmacology},
  • W. Yang, J. Guastella, +9 authors S. Cai
  • Published 2003
  • Medicine, Chemistry
  • British Journal of Pharmacology
  • Caspases play a critical role in apoptosis, and are considered to be key targets for the design of cytoprotective drugs. As part of our antiapoptotic drug‐discovery effort, we have synthesized and characterized Z‐VD‐fmk, MX1013, as a potent, irreversible dipeptide caspase inhibitor. MX1013 inhibits caspases 1, 3, 6, 7, 8, and 9, with IC50 values ranging from 5 to 20 nM. MX1013 is selective for caspases, and is a poor inhibitor of noncaspase proteases, such as cathepsin B, calpain I, or Factor… CONTINUE READING
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