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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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
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Language:English
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Chemistry
Degradation
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container_end_page 13882
container_issue 94
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container_title Chemical communications (Cambridge, England)
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creator 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
description 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.
doi_str_mv 10.1039/d4cc05138f
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subjects Chemistry
Degradation
title Cereblon-recruiting proteolysis targeting chimeras (PROTACs) can determine the selective degradation of HDAC1 over HDAC3
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