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- W2794275020 abstract "660 Cdc25 dual specificity phosphatases are overexpressed in many human tumors and have oncogenic properties. Although several quinone inhibitors of Cdc25 phosphatase have been identified, their selectivity and cellular mechanisms of action have not been fully established. We synthesized and evaluated five novel quinolinedione congeners of a previously reported Cdc25 inhibitor, 6-chloro-7-(2-morpholin-4-yl-ethylamino)-quinoline-5,8-dione (DA3003-1 or NSC 663284). All five quinolinediones inhibited Cdc25A, B and C. The dehalogenated and minimal structure, JUN1111, was a more selective in vitro inhibitor of Cdc25 phosphatases compared with DA3003-1. Like DA3003-1, JUN1111 caused cell cycle arrest and directly inhibited etopically expressed Cdc25B activity in transfected cells. In vitro Cdc25B inhibition by these compounds was sensitive to dithiothreitol concentration, pH, and the presence of glutathione and catalase, suggesting that oxidation was a mechanism for irreversible Cdc25B inactivation. Mass spectrometric analysis showed that the catalytic cysteine of Cdc25B was indeed irreversibly oxidized to its sulfonic acid (SO 3 ) form upon treatment with DA3003-1. DA3003-1 and JUN1111 were also shown to rapidly generate reactive oxygen species in cells, further supporting enzyme inhibition by oxidation. We propose that these quinolinediones regulate the phosphatase activity of Cdc25 through selective and irreversible oxidation at the active site cysteine." @default.
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- W2794275020 date "2005-05-01" @default.
- W2794275020 modified "2023-09-23" @default.
- W2794275020 title "Redox regulation of Cdc25B by novel cell active quinolinediones" @default.
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