1994 Fiscal Year Final Research Report Summary
MULTI-SUBSTRATE TYPE INHIBITORS FOR CDC2 KINASE AND THEIR EVALUATION AS SELECTIVE CELL-CYCLE INHIBITORS
| Project/Area Number |
05671754
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| Research Category |
Grant-in-Aid for General Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Research Field |
Chemical pharmacy
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| Research Institution | KYUSHU UNIVERSITY |
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Principal Investigator |
SASAKI Shigeki KYUSHU UNIVERSITY FACULTY OF PHARMACEUTICAL SCIENCES ASSOCIATE PROFESSOR, 薬学部, 助教授 (10170672)
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| Project Period (FY) |
1993 – 1994
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| Keywords | Protein Kinase / cdc2 kinase / cell cycle / Inhibitor / bisindol / multisubstrate |
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| Research Abstract |
Protein kinases play a significan role in the signal transduction in cell, and are essential enzymes in maintaining norma cell functions. Protein kinases constitue a diverse family of related enzymes, which have similar structures in their catalytic sites. Therefore, it has been a difficult and challenging task to develop their selective inhibitors. We designed new inhibitors which have multisubstrate type structures (IV-VIII), i.e.bisindolylmaleimide for the ATP-binding site of the enzyme, tetrapeptide for the peptide-binding sites, and a spacer linking these units. In the in vitro inhibition assay using activated complex of cdc2 kinase-cycline B,new compounds (Va and VIb) were found to have potent inhibitory activities (Table).
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