Novel non-peptide inhibitors targeting death receptor-mediated apoptosis

Hideaki Kakeya, Yasunobu Miyake, Mitsuru Shoji, Satoshi Kishida, Yujiro Hayashi, Takao Kataoka, Hiroyuki Osada

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

We have previously reported that ECH, (2R, 3R, 4S)-2,3-epoxy-4-hydroxy-5-hydroxymethyl-6-(1E)-propenyl-cyclohex-5-en-1-one inhibits Fas-mediated apoptosis by blocking self-activation of pro-caspase-8 in the death-inducing signaling complex (DISC). A series of ECH derivatives were asymmetrically synthesized via key synthetic intermediates obtained from lipase-catalyzed kinetic resolution. Inhibitory activities of the derivatives towards death receptor-mediated apoptosis both in type I and type II cells were investigated, revealing that novel non-peptide inhibitors, RKTS-33 and RKTS-34, are effective as ECH.

Original languageEnglish
Pages (from-to)3743-3746
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume13
Issue number21
DOIs
Publication statusPublished - 2003 Nov 3

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Kakeya, H., Miyake, Y., Shoji, M., Kishida, S., Hayashi, Y., Kataoka, T., & Osada, H. (2003). Novel non-peptide inhibitors targeting death receptor-mediated apoptosis. Bioorganic and Medicinal Chemistry Letters, 13(21), 3743-3746. https://doi.org/10.1016/j.bmcl.2003.08.003