Design, synthesis, and structure-activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects.

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第一作者： Yasushi,Hattori

第一单位： Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa, 251-8555, Japan. Electronic address: yasushi.hattori@takeda.com.

作者： Yasushi,Hattori ^[1] ; Shigemitsu,Matsumoto ^[2] ; Shinji,Morimoto ^[2] ; Masaki,Daini ^[2] ; Masashi,Toyofuku ^[2] ; Satoru,Matsuda ^[2] ; Rina,Baba ^[2] ; Koji,Murakami ^[2] ; Misa,Iwatani ^[2] ; Hideyuki,Oki ^[2] ; Shinji,Iwasaki ^[2] ; Kouta,Matsumiya ^[2] ; Yusuke,Tominari ^[2] ; Haruhide,Kimura ^[2] ; Mitsuhiro,Ito ^[2]

作者单位： Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa, 251-8555, Japan. Electronic address: yasushi.hattori@takeda.com. ^[1] Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa, 251-8555, Japan. ^[2]

关键词 Drug discovery Epigenetics Hematological side effect LSD1 TAK-418

主题词动物(Animals);酶抑制剂(Enzyme Inhibitors);组蛋白脱甲基酶类(Histone Demethylases);赖氨酸(Lysine);小鼠(Mice);RNA, 信使(RNA, Messenger);构效关系(Structure-Activity Relationship)

DOI 10.1016/j.ejmech.2022.114522

PMID 35749987

发布时间 2022-07-12

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