Novel non-peptide inhibitors targeting death receptor-mediated apoptosis

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

研究成果: Article査読

24 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)3743-3746
ページ数4
ジャーナルBioorganic and Medicinal Chemistry Letters
13
21
DOI
出版ステータスPublished - 2003 11 3

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

フィンガープリント

「Novel non-peptide inhibitors targeting death receptor-mediated apoptosis」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル