Bioorganic Chemistry (2020)
Update date:2022-08-03
Topics:
Satoh, Ryosuke
Hamada, Naoya
Yamada, Ami
Kanda, Yuki
Ishikawa, Fumihiro
Takasaki, Teruaki
Tanabe, Genzoh
Sugiura, Reiko
The recent discovery that an ERK signaling modulator [ACA-28 (2a)] preferentially kills human melanoma cell lines by inducing ERK-dependent apoptosis has generated significant interest in the field of anti-cancer therapy. In the first SAR study on 2a, here, we successfully developed candidates (2b, 2c) both of which induce more potent and selective apoptosis towards ERK-active melanoma cells than 2a, thus revealing the structural basis for inducing the ERK-dependent apoptosis and proposing the therapeutic prospect of these candidates against ERK-dependent cancers represented by melanoma.
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