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Discovery of LWY713 as a potent and selective FLT3 PROTAC degrader with in vivo activity against acute myeloid leukemia.

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第一作者： Wenyan,Liu

第一单位： State Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai, 200032, China.

作者： Wenyan,Liu ^[1] ; Yu,Bai ^[1] ; Licheng,Zhou ^[2] ; Jian,Jin ^[1] ; Meiying,Zhang ^[1] ; Yongxing,Wang ^[3] ; Runfeng,Lin ^[3] ; Weixue,Huang ^[1] ; Xiaomei,Ren ^[1] ; Nan,Ma ^[2] ; Fengtao,Zhou ^[2] ; Zhen,Wang ^[1] ; Ke,Ding ^[4]

作者单位： State Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai, 200032, China. ^[1] International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, 855 Xingye Avenue East, Guangzhou, 511400, China. ^[2] Livzon Research Institute, Livzon Pharmaceutical Group Inc., #38 Chuangye North Road, Jinwan District, Zhuhai, 519000, China. ^[3] State Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai, 200032, China; International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, 855 Xingye Avenue East, Guangzhou, 511400, China; Institute of Basic Medicine and Cancer (IBMC), Chinese Academy of Sciences, Hangzhou, Zhejiang, 310022, China. Electronic address: dingk@sioc.ac.cn. ^[4]

关键词 Acute myeloid leukemia Antitumor activity Degrader FLT3 Proteolysis targeting chimera