Cited by 120Histone Deacetylase Inhibitors ResearchEpigenetics and DNA MethylationProtein Degradation and Inhibitors

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HDAC inhibitors still need a home run, despite recent approval

Guha, Malini·2015·Nature Reviews Drug Discovery

DOI 10.1038/nrd4583

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Background
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The Roadmap Epigenomics Project opens new drug development avenues
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“The anticancer mechanisms of HDACis also need further research [26].”
Background
HDAC5 Inhibits Hepatic Lipogenic Genes Expression by Attenuating the Transcriptional Activity of Liver X Receptor
Jia, H.-Y., Li, Q., & Lv, L.-F. (2016) · Cellular Physiology and Biochemistry · doi:10.1159/000447858 · Cited by 18
Updates in pathobiological aspects of anaplastic large cell lymphoma
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“HDAC inhibitors have already been approved by the Food and Drug Administration (FDA) for the treatment of T-cell malignancies (73 – 75).”
Background
Design, synthesis and biological evaluation of novel histone deacetylase inhibitors incorporating 4-aminoquinazolinyl systems as capping groups
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“HDAC inhibitors (HDACIs) have been identified as anticancer agents (Drummond et al., 2005; Guha, 2015; Mottamal, Zheng, Huang, & Wang, 2015; Qiao et al., 2013), immune modulators (Adcock, Ito, & Barnes, 2005; Choi & Reddy, 2011; Dinarello, Fossati, & Mascagni, 2011; Faraco, Cavone, & Chiarugi,…”
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“In general, HDACIs are unable to speciﬁcally target certain isoforms in the subclass of HDACs [150].”
Background
Novel hydroxamic acids incorporating 1-((1H-1,2,3-Triazol-4-yl)methyl)-3-hydroxyimino-indolin-2-ones: synthesis, biological evaluation, and SAR analysis
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Antiandrogen-Equipped Histone Deacetylase Inhibitors Selectively Inhibit Androgen Receptor (AR) and AR-Splice Variant (AR-SV) in Castration-Resistant Prostate Cancer (CRPC)
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“It has been reported that limited penetration and extensive tissue distribution result in clinical ineffectiveness and off-target effects, such as myelosuppression, fatigue, and cardiac toxicity [9].”
Background
Quantitative Acetylomics Uncover Acetylation-Mediated Pathway Changes Following Histone Deacetylase Inhibition in Anaplastic Large Cell Lymphoma
Zrimšek, M., Kuchaříková, H., Draganić, K., Dobrovolná, P., Spornberger, V. H., Winkelmayer, L., Hassler, M. R., Lochmanová, G., Zdráhal, Z., & Egger, G. (2022) · Cells · doi:10.3390/cells11152380 · Cited by 9
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Erratum: HDAC inhibitors still need a home run, despite recent approval
Guha, M. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4632 · Cited by 8
Self-citation
Screening of histone deacetylase 1 inhibitors in natural products by capillary electrophoresis
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Class I and II Histone Deacetylase Inhibitor LBH589 Promotes Endocrine Differentiation in Bone Marrow Derived Human Mesenchymal Stem Cells and Suppresses Uncontrolled Proliferation
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Yang, L., Ding, R., Tong, X., Shen, T., Jia, S., Yan, X., Zhang, C., & Wu, L. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.117029 · Cited by 5
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Authors: Guha, M.
Corresponding author: Guha, Malini
Venue: Nature Reviews Drug Discovery
Publisher: Springer Science and Business Media LLC
Published: 2015-04
Volume: 14
Issue: 4
Pages: 225-226
ISSN: 1474-1776 (ISSN-L)
1474-1784
DOI: 10.1038/nrd4583
OpenAlex: W2033780602
Cited by: 120
References: 0
Citations by year: 2026: 5 · 2025: 3 · 2024: 8 · 2023: 9 · 2022: 8 · 2021: 14 · 2020: 18 · 2019: 11 · 2018: 9 · 2017: 16 · 2016: 12 · 2015: 7
Type: other
Language: en
Update notices: erratum (2015-04-30)
Open access: closed
Licence: www.springer.com/tdm (tdm)
www.springer.com/tdm (vor)
Locations: Nature Reviews Drug Discovery (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Histone Deacetylase Inhibitors Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
Keywords: histone deacetylase inhibitors, epigenetic regulators, cancer therapy, drug approval
MeSH terms: Histone Deacetylases, Humans, Multiple Myeloma, United States, United States Food and Drug Administration, Drug Approval, Epigenesis, Genetic, Histone Deacetylase Inhibitors

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