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.
申请公布号
WO2008070823(A3)
申请公布日期
2008.12.11
申请号
WO2007US86751
申请日期
2007.12.07
申请人
UNIVERSITY OF SOUTH FLORIDA;YALE UNIVERSITY;SEBTI, SAID, M.;CHENG, JIN, Q.;HAMILTON, ANDREW, D.;KAYSER, KATHERINE