Structure‐Guided Optimization of a Molecular Glue Targeting the KBTBD4‐HDAC1/2 Complex
Optimization of UM171, a molecular glue initiating the degradation of neosubstrate HDAC1/2–CoREST–LSD1 through a multiprotein complex formed with KBTBD4, resulted in a 20‐fold improvement in glue activity, demonstrated by the stability of its ternary complex with KBTBD4‐HDAC2.
Timea Baló, Zhuoyao Chen, Laurine Palluaud et al.
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