Bisubstrate Analog Inhibitors for Protein Kinases

A new approach for the design of protein kinase inhibitors is disclosed. Using this approach a potent insulin receptor protein tyrosine kinase inhibitor has been produced. In principle, this method is general and could be applied to any protein kinase. Previous bisubstrate analog compounds have been weak protein kinase inhibitors. The design of protein kinase bisubstrate/transition state analog inhibitors is based on the concept of phosphoryl transfer mechanism involving. Based on this idea, the distance between the entering nucleophile and the gamma-phosphate of ATP in the enzyme active site should be at least 4.9 angstroms. Furthermore, a proton released from the tyrosine phenol appears to be late in the mechanism so that a hydrogen bond formed between the attacking tyrosine phenol and an active site aspartate residue would be maintained. Based on this idea, a bisubstrate analog was synthesized as a peptide ATP conjugate for the insulin receptor tyrosine kinase. Patent (Set) aban WO 01/70770; 7,045,617

US 7,045,617

Inventor(s): Parang, Keykavous

Type of Offer: Licensing

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