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Updated: Aug 16, 2025

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
Published on: August 10, 2017
A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting
Jasmine M Cross1, Megan E Coulson1,2, Joshua P Smalley1
1Leicester Institute of Structural and Chemical Biology, School of Chemistry, University of Leicester Leicester LE1 7RH UK JTHodgkinson@le.ac.uk.
Abstract:
Click chemistry was utilised to prepare a library of PROTACs based on entinostat a class I histone deacetylase (HDAC) inhibitor in clinical trials. A novel PROTAC JMC-137 was identified as a HDAC1/2 and HDAC3 degrader in HCT116 cells. However, potency was compromised compared to previously identified class I HDAC PROTACs highlighting the importance in the choice of HDAC ligand, functional group for linker attachment and positioning in PROTAC design.
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