Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: Insights into specificity and potency

[摘要] 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. (C) 1999 Elsevier Science Ltd. All rights reserved.

[发布日期] 1999-12-06