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ID: ALA4184246

Journal: Bioorg Med Chem Lett

Title: Semisynthesis and biological evaluation of a cotylenin A mimic derived from fusicoccin A.

Authors: Inoue T, Higuchi Y, Yoneyama T, Lin B, Nunomura K, Honma Y, Kato N.

Abstract: In an effort to overcome the unavailability of cotylenin A (CN A), an anticancer agent and a stabilizer of protein-protein interactions (PPIs) mediated by 14-3-3 proteins, ISIR-050 was designed as a CN A mimic. The synthesis was accomplished via a semisynthetic approach starting from fusicoccin A. ISIR-050 showed interferon-α (IFNα)-dependent growth inhibitory activity and a PPI stabilization effect similar to those of CN A. The biochemical analysis suggested that ISIR-050 and CN A induce the same pharmacological response to IFNα-treated cancer cells and that 14-3-3 proteins play a role in the mode of action.

CiteXplore: 29398541

DOI: 10.1016/j.bmcl.2018.01.030