Ontology highlight
ABSTRACT:
SUBMITTER: Kim YB
PROVIDER: S-EPMC4176526 | biostudies-literature | 2014 Oct
REPOSITORIES: biostudies-literature
Kim Young B YB Kang Chang Won CW Ranatunga Sujeewa S Yang Hua H Sebti Said M SM Del Valle Juan R JR
Bioorganic & medicinal chemistry letters 20140828 19
We report the design, synthesis, and biological evaluation of imidazopyridine-based peptidomimetics based on the substrate consensus sequence of Akt, an AGC family serine/threonine kinase hyperactivated in over 50% of human tumors. Our ligand-based approach led to the identification of novel substrate mimetic inhibitors of Akt1 featuring an unnatural extended dipeptide surrogate. Compound 11 inhibits Akt isoforms in the sub-micromolar range and exhibits improved proteolytic stability relative to ...[more]