Cereblon-recruiting proteolysis targeting chimeras (PROTACs) can determine the selective degradation of HDAC1 over HDAC3

Histone deacetylase (HDAC) enzymes 1-3 exist in several corepressor complexes and are viable drug targets. To date, proteolysis targeting chimeras (PROTACs) designed to target HDAC1-3 typically exhibit the selective degradation of HDAC3. Herein, we report cereblon-recruiting PROTACs that degrade HDA...

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Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2024-11, Vol.6 (94), p.13879-13882
Main Authors: Pavan, Aline R, Smalley, Joshua P, Patel, Urvashi, Pytel, Wiktoria A, dos Santos, Jean Leandro, Cowley, Shaun M, Schwabe, John W. R, Hodgkinson, James T
Format: Article
Language:English
Subjects:
Chemistry
Degradation
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Summary:Histone deacetylase (HDAC) enzymes 1-3 exist in several corepressor complexes and are viable drug targets. To date, proteolysis targeting chimeras (PROTACs) designed to target HDAC1-3 typically exhibit the selective degradation of HDAC3. Herein, we report cereblon-recruiting PROTACs that degrade HDAC1 with selectivity over HDAC3. Cereblon-recruiting PROTACs can degrade HDAC1 with selectivity over HDAC3.
ISSN:1359-7345
1364-548X
1364-548X
DOI:10.1039/d4cc05138f