Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1359526 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
Abstract
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 a parent pentapeptide.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Young B. Kim, Chang Won Kang, Sujeewa Ranatunga, Hua Yang, Said M. Sebti, Juan R. Del Valle,