Said M. Sebti,Jin Q. Cheng,Andrew D. Hamilton,Katherine Kayser-Bricker
申请号：
US12480329
公开号：
US08822524B2
申请日:
2009.06.08
申请国别(地区):
US
年份:
2014
代理人:
摘要：
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.
