| Budget Amount *help |
¥2,100,000 (Direct Cost: ¥2,100,000)
Fiscal Year 1994: ¥600,000 (Direct Cost: ¥600,000)
Fiscal Year 1993: ¥1,500,000 (Direct Cost: ¥1,500,000)
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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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