2. Academic Validation
  3. Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency

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

  • Bioorg Med Chem Lett. 1999 Dec 6;9(23):3335-40. doi: 10.1016/s0960-894x(99)00612-5.
K B Kim 1,  J Myung,  N Sin,  C M Crews
Affiliations

Affiliation

  • 1 Department of Molecular, Cellular, and Developmental Biology, Yale University, New Haven, CT 06520-8103, USA.
PMID: 10612595 DOI: 10.1016/s0960-894x(99)00612-5
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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