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Some natural flavonoids are competitive inhibitors of Caspase-1, -3 and -7 despite their cellular toxicity
Authors:White J Brandon  Beckford Jeremy  Yadegarynia Sina  Ngo Nhi  Lialiutska Tetiana  d'Alarcao Marc
Affiliation:a Department of Biological Sciences, San José State University, One Washington Square, San Jose, CA 95192-0100, United States
b Department of Chemistry, San José State University, One Washington Square, San Jose, CA 95192-0101, United States
Abstract:A common feature of both apoptosis and inflammation is the activation of caspases. Caspases are aspartate-directed cysteine proteases that have numerous cellular targets. It has been discovered that several flavonoids are inhibitors of caspases. Flavonoids are members of a family of polyphenolic compounds from plants that have many biological properties, one of which is the ability to induce cell death. Some flavonoids are selective inhibitors of particular caspases. Since some of the inhibitory flavonoids are nevertheless cytotoxic, these results suggest that flavonoid-induced cell death may be occurring through a non-classical apoptosis pathway that is not dependent on caspase activity.
Keywords:Apoptosis  Caspase  Flavonoid  Breast cancer  Enzyme kinetics  Small molecule inhibitor
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