Dual-specificity phosphatase CDC25A/B inhibitor identified from a focused library with nonelectrophilic core structure

Ayako Tsuchiya, Go Hirai, Yusuke Koyama, Kana Oonuma, Yuko Otani, Hiroyuki Osada, Mikiko Sodeoka

Research output: Contribution to journalArticlepeer-review

21 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)294-298
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume3
Issue number4
DOIs
Publication statusPublished - Apr 12 2012
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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