Cited by 163Histone Deacetylase Inhibitors ResearchEnzyme function and inhibitionEpigenetics and DNA Methylation

Development of a histone deacetylase 6 inhibitor and its biological effects

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Lee, Ju-Hee, Mahendran, Adaickapillai, Yao, Yuanshan, Ngo, Lang, Venta-Perez, Gisela, Choy, Megan L., Kim, Nathaniel, Ham, Won-Seok +2 more·2013·Proceedings of the National Academy of Sciences

Abstract

Significance: We discovered a hydroxamic acid-based small-molecule N -hydroxy-4-(2-[(2-hydroxyethyl)(phenyl)amino]-2-oxoethyl)benzamide selectively inhibits histone deacetylase 6 catalytic activity in vivo and in vitro.

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Crossref · 10.1073/pnas.1313893110

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  • HPOB potency against HDAC6 is comparable to SAHA-like inhibitors, but its potency against other isozymes is significantly reduced.

    “Accordingly, the potency of HPOB against HDAC6 is comparable to SAHA-like inhibitors, but HPOB potency against other isozymes is significantly reduced.43”

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Authors
Lee, J.-H., Mahendran, A., Yao, Y., Ngo, L., Venta-Perez, G., Choy, M. L., Kim, N., Ham, W.-S., Breslow, R., & Marks, P. A.
Affiliations
  • Memorial Sloan Kettering Cancer Center (US)
  • Columbia University (US)
Corresponding author
Marks, Paul A.
Venue
Proceedings of the National Academy of Sciences
Published
2013-09-10
Volume
110
Issue
39
Pages
15704-15709
ISSN
  • 0027-8424 (ISSN-L)
  • 1091-6490
OpenAlex
W2148383035
Cited by
141
References
28
Citations by year
2026: 5 · 2025: 7 · 2024: 6 · 2023: 7 · 2022: 7 · 2021: 15 · 2020: 15 · 2019: 17 · 2018: 16 · 2017: 12 · 2016: 14 · 2015: 13 · 2014: 7
FWCI
5.53
Type
journal article
Language
en
Open access
Locations
  • Proceedings of the National Academy of Sciences (publishedVersion)
  • Europe PMC (PubMed Central) (publishedVersion)
  • PubMed Central (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • Servier
  • National Cancer Institute (P30CA08748-44, P30CA008748)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Histone Deacetylase Inhibitors Research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Enzyme function and inhibition
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
Keywords
HDAC6, HDAC6 inhibitors, isoform-selective inhibition, hydroxamic acids, DNA-damaging agents, growth inhibition, small molecule inhibitors
MeSH terms
Vorinostat, Acetylation, Animals, Antineoplastic Agents, Autophagy, Cell Line, Transformed, Cell Survival, Doxorubicin, Etoposide, Histone Deacetylases, Histones, Humans, Hydroxamic Acids, Trehalose, Tubulin, Apoptosis, Xenograft Model Antitumor Assays, Cell Line, Tumor, Mice, DNA Breaks, Double-Stranded, Histone Deacetylase Inhibitors

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