Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure |
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| Authors: | Tsuchiya Ayako Hirai Go Koyama Yusuke Oonuma Kana Otani Yuko Osada Hiroyuki Sodeoka Mikiko |
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| Institution: | †RIKEN
Advanced
Science Institute, 2-1 Hirosawa, Wako-shi, Saitama 351-0198, Japan;‡Sodeoka Live Cell Chemistry Project, ERATO, Japan Science and Technology Agency, 2-1 Hirosawa, Wako-shi, Saitama 351-0198, Japan |
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| Abstract: | Focused libraries of enamine derivatives with a nonacidic, nonelectrophilic core structure were screened for inhibitors of dual-specificity protein phosphatases, and an o-hydroxybenzyl derivative RE44 (10d) was identified as a selective inhibitor of CDC25A/B. This inhibitor induced cell-cycle arrest of tsFT210 cells at the G2/M phase and inhibited dephosphorylation of the CDC25B substrate CDK1. Unlike most quinone-based inhibitors, 10d does not generate reactive oxygen species. |
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| Keywords: | dual-specificity protein phosphatases CDC25 inhibitor reactive oxygen species cell cycle focused library |
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