Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure

[Image: see text] 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...

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Autores principales: Tsuchiya, Ayako, Hirai, Go, Koyama, Yusuke, Oonuma, Kana, Otani, Yuko, Osada, Hiroyuki, Sodeoka, Mikiko
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2012
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3324983/
https://www.ncbi.nlm.nih.gov/pubmed/22506091
http://dx.doi.org/10.1021/ml2002778
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author Tsuchiya, Ayako
Hirai, Go
Koyama, Yusuke
Oonuma, Kana
Otani, Yuko
Osada, Hiroyuki
Sodeoka, Mikiko
author_facet Tsuchiya, Ayako
Hirai, Go
Koyama, Yusuke
Oonuma, Kana
Otani, Yuko
Osada, Hiroyuki
Sodeoka, Mikiko
author_sort Tsuchiya, Ayako
collection PubMed
description [Image: see text] 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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spelling pubmed-33249832012-04-13 Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure Tsuchiya, Ayako Hirai, Go Koyama, Yusuke Oonuma, Kana Otani, Yuko Osada, Hiroyuki Sodeoka, Mikiko ACS Med Chem Lett [Image: see text] 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. American Chemical Society 2012-02-15 /pmc/articles/PMC3324983/ /pubmed/22506091 http://dx.doi.org/10.1021/ml2002778 Text en Copyright © 2012 American Chemical Society Terms of Use (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html)
spellingShingle Tsuchiya, Ayako
Hirai, Go
Koyama, Yusuke
Oonuma, Kana
Otani, Yuko
Osada, Hiroyuki
Sodeoka, Mikiko
Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure
title Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure
title_full Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure
title_fullStr Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure
title_full_unstemmed Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure
title_short Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure
title_sort dual-specificity phosphatase cdc25a/b inhibitor identified from a focused library with nonelectrophilic core structure
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3324983/
https://www.ncbi.nlm.nih.gov/pubmed/22506091
http://dx.doi.org/10.1021/ml2002778
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