Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure |
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Authors: | S Sasaki T Hashimoto N Obana H Yasuda Y Uehara M Maeda |
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Affiliation: | Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan. |
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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. |
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