Cited by 129Protein Degradation and InhibitorsHistone Deacetylase Inhibitors ResearchChemical Synthesis and Analysis

PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes

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Smalley, Joshua P., Adams, Grace E., Millard, Christopher J., Song, Yun, Norris, James K. S., Schwabe, John W. R., Cowley, Shaun Michael, Hodgkinson, James T.·2020·Chemical Communications

Abstract

We have identified a proteolysis targeting chimera (PROTAC) of class I HDACs 1, 2 and 3. Our PROTAC decreased HDAC 1, 2 & 3 protein abundance, increased histone acetylation levels and compromised colon cancer HCT116 cell viability.

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Authors
Smalley, J. P., Adams, G. E., Millard, C. J., Song, Y., Norris, J. K. S., Schwabe, J. W. R., Cowley, S. M., & Hodgkinson, J. T.
Affiliations
University of Leicester (GB)
Corresponding author
  • Schwabe, John W. R.
  • Cowley, Shaun Michael
  • Hodgkinson, James T.
Venue
Chemical Communications
Published
2020
Volume
56
Issue
32
Pages
4476-4479
ISSN
  • 1359-7345 (ISSN-L)
  • 1364-548X
OpenAlex
W3011997563
Cited by
121
References
31
Citations by year
2026: 8 · 2025: 19 · 2024: 17 · 2023: 21 · 2022: 24 · 2021: 16 · 2020: 16
FWCI
6.62
Type
journal article
Language
en
Open access
Locations
  • Chemical Communications (publishedVersion)
  • PubMed (publishedVersion)
  • PubMed Central (acceptedVersion)
  • Figshare (submittedVersion, cc-by)
Funders
  • Engineering and Physical Sciences Research Council (EP/S030492/1)
  • Medical Research Council ((MR/J009202/1))
  • Wellcome Trust (Senior Investigator Award (100237/ Z/12/Z))
  • Biotechnology and Biological Sciences Research Council ((BB/N002954/1), (BB/P021689/1))
  • Royal Society (Wolfson Research Merit Award.)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Histone Deacetylase Inhibitors Research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
Keywords
PROTACs, class I histone deacetylases, HDAC1, HDAC2, HDAC3, protein degradation, corepressor complex, histone acetylation, colon cancer, HCT116 cells
MeSH terms
Animals, Antineoplastic Agents, Cell Survival, Histone Deacetylases, Humans, Cell Line, Tumor, Mice, Histone Deacetylase 1, Histone Demethylases, Histone Deacetylase Inhibitors, Co-Repressor Proteins, Proteolysis

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