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

doi:10.1016/S0960-894X(98)00163-2

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

Chemo-Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-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 language	English
Pages (from-to)	1019-1022
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	8
Issue number	9
DOIs	https://doi.org/10.1016/S0960-894X(98)00163-2
Publication status	Published - May 1998

All Science Journal Classification (ASJC) codes

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

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10.1016/S0960-894X(98)00163-2

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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.",

author = "Shigeki Sasaki and Tomohiro Hashimoto and Norihiro Obana and Hideyo Yasuda and Yoshimasa Uehara and Minoru Maeda",

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AU - Sasaki, Shigeki

AU - Hashimoto, Tomohiro

AU - Obana, Norihiro

AU - Yasuda, Hideyo

AU - Uehara, Yoshimasa

AU - Maeda, Minoru

PY - 1998/5

Y1 - 1998/5

N2 - 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.

AB - 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.

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IS - 9

ER -

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

Abstract

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