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Development of a histone deacetylase 6 inhibitor and its biological effects
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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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“Accordingly, the potency of HPOB against HDAC6 is comparable to SAHA-like inhibitors, but HPOB potency against other isozymes is significantly reduced.43”
From Histone deacetylase 6 structure and molecular basis of catalysis and inhibition (2016) · cites this paper as [43]
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Metadata
- 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
- Publisher
- National Academy of Sciences
- Published
- 2013-09-10
- Volume
- 110
- Issue
- 39
- Pages
- 15704-15709
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- PMC
- PMC3785767
- 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
- bronze
- doi.org
- 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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