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August 20, 2025Open Access

Targeted histone deacetylase degradation via chemical induced proximity by direct recruitment of the CUL4 complex adaptor protein DDB1

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Authors

SZShiyang ZhaiNWNicola WillemsenTSTao Sun

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Overview

Targeted protein degradation improves HDAC elimination in multiple myeloma, suggesting new treatment avenues.

Key Points

  • SZ-2 led to effective degradation of HDAC1, demonstrating a promising approach in treating multiple myeloma.
  • The E3 ligase complex CUL4-DDB1-CRBN was employed to facilitate selective protein degradation.
  • By binding both DDB1 and HDACs, SZ-2 shows potential as a novel therapeutic agent in cancer treatment.
  • Further exploration of targeted degradation strategies may enhance treatment outcomes for various cancers.

Cite This Study

Zhai et al. (2025) studied this question.

synapsesocial.com/papers/68af750c7567bf4f94fedde7https://doi.org/10.26434/chemrxiv-2025-1bqnv
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  5. 5Temporal and Spatial Characterization of CUL3<sup>KLHL20</sup>-Driven Targeted Degradation of BET Family BRD Proteins by the Macrocycle-Based Degrader BTR20042025