Development of a Water-Soluble Indolylmaleimide Derivative
IM-93 Showing Dual Inhibition of Ferroptosis and NETosis
Version 4 2019-09-10, 13:39
Version 3 2019-08-06, 10:03
Version 2 2019-08-05, 22:29
Version 1 2019-08-02, 15:44
Posted on 2019-09-10 - 13:39
The
indolylmaleimide (IM) derivative IM-17 shows inhibitory
activity against oxidative-stress-induced necrotic cell death and
cardioprotective activity in rat ischemia-reperfusion injury models.
In order to develop a more potent derivative, we conducted a detailed
structure–activity relationship study of IM derivatives and
identified IM-93 as the most potent derivative with good
water solubility. IM-93 inhibited ferroptosis and NETosis,
but not necroptosis or pyroptosis. In contrast, ferrostatin-1 (Fer-1),
a ferroptosis inhibitor, did not inhibit NETosis, although the accompanying
lipid peroxidation was partially inhibited by Fer-1, as well as by IM-93. Thus, IM derivatives have a unique activity profile
and appear to be promising candidates for in vivo application.
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Dodo, Kosuke; Kuboki, Erika; Shimizu, Tadashi; Imamura, Ryu; Magarisawa, Megumi; Takahashi, Masahiro; et al. (2019). Development of a Water-Soluble Indolylmaleimide Derivative
IM-93 Showing Dual Inhibition of Ferroptosis and NETosis. ACS Publications. Collection. https://doi.org/10.1021/acsmedchemlett.9b00142
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AUTHORS (14)
KD
Kosuke Dodo
EK
Erika Kuboki
TS
Tadashi Shimizu
RI
Ryu Imamura
MM
Megumi Magarisawa
MT
Masahiro Takahashi
TT
Takuto Tokuhiro
SY
Satoshi Yotsumoto
KA
Kenichi Asano
SN
Shuhei Nakao
NT
Naoki Terayama
TS
Takashi Suda
MT
Masato Tanaka
MS
Mikiko Sodeoka