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  • Title: Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency.
    Author: Kim KB, Myung J, Sin N, Crews CM.
    Journal: Bioorg Med Chem Lett; 1999 Dec 06; 9(23):3335-40. PubMed ID: 10612595.
    Abstract:
    While two structurally related epoxyketone-containing antitumor natural products, epoxomicin and eponemycin, share the proteasome as a common intracellular target, they differ in their antiproliferative activity, proteasome subunit binding specificity, and rates of proteasome inhibition. As a first step towards understanding such differences and developing novel proteasome subunit-specific inhibitors, we report here the synthesis and characterization of epoxomicin/dihydroeponemycin chimerae.
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