The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
May. 16, 2006
Filed:
Mar. 21, 2001
Philip A. Cole, Baltimore, MD (US);
Keykavous Parang, Narragansett, RI (US);
Ararat Abloogu, New York, NY (US);
Ronald A. Kohanski, Fair Lawn, NJ (US);
Aliya Courtney, Baltimore, MD (US);
Philip A. Cole, Baltimore, MD (US);
Keykavous Parang, Narragansett, RI (US);
Ararat Abloogu, New York, NY (US);
Ronald A. Kohanski, Fair Lawn, NJ (US);
Aliya Courtney, Baltimore, MD (US);
Mount Sinai School of Medicine, New York, NY (US);
Johns Hopkins University, Baltimore, MD (US);
Abstract
Protein kinase inhibitors have applications as anti-cancer therapeutic agents and biological tools in cell signalling. Potent and selective bisubstrate inhibitors for the insulin receptor tyrosine kinase are based on a phosphoryl transfer mechanism involving a dissociative transition state. One such inhibitor is synthesized by linking ATPγS to a peptide substrate analog via a two-carbon spacer. The compound is a high-affinity competitive inhibitor against both nucleotide and peptide substrate and shows a slow off-rate. A crystal structure of this inhibitor bound to the tyrosine kinase domain of the insulin receptor confirms the key design features inspired by a dissociative transition state, and reveal that the linker takes part in the octahedral coordination of an active site Mgion.