Asymmetric Engagement of Dimeric CRL3KBTBD4by the Molecular Glue UM171 Licenses Degradation of HDAC1/2 Complexes
Megan JR Yeo,
Olivia Zhang,
Xiaowen Xie
et al.
Abstract:UM171 is a potent small molecule agonist of ex vivo human hematopoietic stem cell (HSC) self-renewal, a process that is tightly controlled by epigenetic regulation. By co-opting KBTBD4, a substrate receptor of the CULLIN3-RING E3 ubiquitin ligase complex, UM171 promotes the degradation of members of the CoREST transcriptional corepressor complex, thereby limiting HSC attrition. However, the direct target and mechanism of action of UM171 remain unclear. Here, we reveal that UM171 acts as a molecular glue to ind… Show more
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