Substrate-mimetic Akt inhibitor

US8822524B2 · kind B2 · utility

Assignees

• University of South Florida · US
• Yale University · US

Inventors

• Said M. Sebti · Tampa, US
• Jin Q. Cheng · Tampa, US
• Andrew D. Hamilton · Felton, GB
• Katherine J. Kayser-Bricker · Branford, US

Key dates

• Filing date: Jun 8, 2009
• Grant date: Sep 2, 2014
• Expiry date: Dec 29, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/16
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.