Article
Discovery of LWY713 as a potent and selective FLT3 PROTAC degrader with in vivo activity against acute myeloid leukemia.
European journal of medicinal chemistry - 15 Jan 2024
Liu Wenyan, Bai Yu, Zhou Licheng, Jin Jian, Zhang Meiying, Wang Yongxing, Lin Runfeng, Huang Weixue, Ren Xiaomei, Ma Nan, Zhou Fengtao, Wang Zhen, Ding Ke
Abstract excerpt
Fms-like tyrosine kinase 3 (FLT3) has been validated as a therapeutic target for acute myeloid leukemia (AML). While a number of FLT3 kinase inhibitors have been approved for AML treatment, the clinical data revealed that they cannot achieve complete and sustained suppression of FLT3 signaling at the tolerated dose. Here we report a series of new, potent and selective FLT3 proteolysis targeting chimera degraders....
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