Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure

Shigeki Sasaki, Tomohiro Hashimoto, Norihiro Obana, Hideyo Yasuda, Yoshimasa Uehara, Minoru Maeda

Research output: Contribution to journalArticlepeer-review

18 Citations (Scopus)

Abstract

New inhibitors have been designed for cdc2 kinase based on a multiple pseudosubstrate structure. The new inhibitors have three different structural components: 3,4-bis(indol-3-yl)maleimide, Ac-Cys-(Ser)-Pro-Lys-Lys-NHMe, and ethyloxy group between the two components. Inhibitory activities toward cdc2 and other protein kinases were investigated, and the compound (21) with Ac- Cys-Pro-Lys-Lys-NHMe connected with the triethylene glycol spacer exhibited the most potent inhibition with relatively high selectivity.

Original languageEnglish
Pages (from-to)1019-1022
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume8
Issue number9
DOIs
Publication statusPublished - May 1 1998

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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