Targeted Protein Degradation of Histone Deacetylases by Hydrophobically Tagged Inhibitors
ACS Medicinal Chemistry Letters(2023)
摘要
There is a growing interest in alternative strategies for targeted protein degradation. In this work, we present the development of histone deacetylase (HDAC) degraders based on hydrophobic tagging technology. To this end, a library of hydro-phobically tagged HDAC inhibitors was synthesized via efficient solid-phase protocols utilizing pre-loaded resins. The subsequent biological evaluation led to the identification of our best degrader, 1a, which significantly decreased HDAC1 levels in MM.1S multiple myeloma cells.
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关键词
Hydrophobic tagging,targeted protein degradation,histone deacetylase,solid-phase synthesis
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