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Caspase-3 (CASP3; CPP32)

In vitro studies identified specific CASP3 inhibitors that could help determine the protein's role in cancer and other diseases. Inhibition of individual caspases has only been effective with genetic knockdown methods. In enzymatic assays, optimized, peptide-based CASP3 inhibitors had subnanomolar potency and more than 120-fold selectivity over the structurally related CASP7 (MCH3). In a human cervical cancer cell line, a cell-permeable variant of one of the identified compounds selectively inhibited active CASP3 and decreased viability compared with a pan-caspase inhibitor. Next steps could include evaluating the inhibitors in animal models of cancer.

SciBX 6(35); doi:10.1038/scibx.2013.954
Published online Sept. 12, 2013

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Vickers, C.J. et al. J. Am. Chem. Soc.; published online Aug. 5, 2013;
Contact: Dennis W. Wolan, The Scripps Research Institute, La Jolla, Calif.