936571-58-3Relevant academic research and scientific papers
SUBSTRATE-MIMETIC AKT INHIBITOR
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Page/Page column 4; 10-11; 4/14, (2008/12/06)
Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with 0 a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionallv 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 counterpartsand are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.
Modifications of the GSK3β substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics
Kayser, Katherine J.,Glenn, Matthew P.,Sebti, Said M.,Cheng, Jin Q.,Hamilton, Andrew D.
, p. 2068 - 2073 (2007/10/03)
Amplification, overexpression, and elevated activation of Akt have been detected in many human malignancies making it an important target for cancer therapy. The Akt substrate-binding site offers a large number of potential interactions to an appropriatel
