Discovery of Selective and Potent ATR Degrader for Exploration its Kinase‐Independent Functions in Acute Myeloid Leukemia Cells
Yubo Wang,
Ruonan Wang,
Yanli Zhao
et al.
Abstract:ATR has emerged as a promising target for anti‐cancer drug development. Several potent ATR inhibitors are currently undergoing various stages of clinical trials, but none have yet received FDA approval due to unclear regulatory mechanisms. In this study, we discovered a potent and selective ATR degrader. Its kinase‐independent regulatory functions in acute myeloid leukemia (AML) cells were elucidated using this proteolysis‐targeting chimera (PROTAC) molecule as a probe. The ATR degrader, 8i, exhibited signific… Show more
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