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Bioorg Med Chem Lett. 1999 Dec 6;9(23):3335-40.

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

Author information

1
Department of Molecular, Cellular, and Developmental Biology, Yale University, New Haven, CT 06520-8103, USA.

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.

PMID:
10612595
DOI:
10.1016/s0960-894x(99)00612-5
[Indexed for MEDLINE]

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