A61K 31/404(20130101), A61K 31/132(20130101), C07D 209/04(20130101), C07C 255/50(20130101), C07C 255/51(20130101)
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.
Sebti, Said M.; Cheng, Jin Q.; Hamilton, Andrew D.; and Kayser-Bricker, Katherine, "Substrate-mimetic Akt inhibitor" (2014). USF Patents. 155.
University of South Florida Yale University