635678-67-0Relevant academic research and scientific papers
Novel non-peptide inhibitors targeting death receptor-mediated apoptosis
Kakeya, Hideaki,Miyake, Yasunobu,Shoji, Mitsuru,Kishida, Satoshi,Hayashi, Yujiro,Kataoka, Takao,Osada, Hiroyuki
, p. 3743 - 3746 (2003)
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.
