Cyclin Based Inhibitors of CDK2 and CDK4

摘要

Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.

主权项

1. A synthetic CDK/cyclin inhibitor that inhibits interaction of a complex formed between a first CDK protein and a first cyclin protein with a substrate of the complex, the synthetic CDK/cyclin inhibitor comprising 1-(3,5-dichlorophenyl)-5-methyl-1H-1,2,4-triazole carboxamide at the N-terminal, the inhibitor comprising βHomoLeu-NMethylPhe-NH2 at the C-terminal, and the inhibitor comprising a linking group between the N-terminal and the C-terminal, the linking group comprising arginine or an arginine isostere.