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HDAC inhibitors still need a home run, despite recent approval
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“Importantly, dose-limiting adverse effects such as cardiac toxicity associated with hERG K+ channel activation are hindering their progress in the clinic [133, 134].”
From Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies (2020) · cites this paper as [133]
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Items 101–117 of 117
Shirbhate, E., Pandey, J., Patel, V. K., Veerasamy, R., & Rajak, H. (2022) · Turkish Journal of Pharmaceutical Sciences · doi:10.4274/tjps.galenos.2022.12269 · Cited by 4
Ali, F. E., Abdelhafez, A. H., Rabea, S. M., Alzahrani, A. Y. A., Mohammed, A. F., & Youssif, B. G. M. (2026) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2026.145800 · Cited by 4
Quoc, T. N., Nga, N. T., Kim, J. S., Kim, H. K., Kim, J., Kang, J. S., Tùng, T. T., Dung, D. T. M., Anh, D. T., Han, S., et al. (2024) · New Journal of Chemistry · doi:10.1039/d4nj03452j · Cited by 3
Thanh, T. D., Thach, V. X., Cuong, H. D., Chinh, L. V., Dung, N. T., Thảo, Đ. T., Quy, D. Q., The, H., & Vu, T. K. (2025) · ChemistrySelect · doi:10.1002/slct.202405219 · Cited by 2
Computational Structure–Activity Relationship Studies of Epigenetic Target Inhibitors
Méndez‐Lucio, O. (2016) · Elsevier eBooks · doi:10.1016/b978-0-12-802808-7.00013-7 · Cited by 2
Song, C., Lin, Y., Cai, C., Tao, K., Tan, J., Xiong, K., Yang, W., Chi, J., Peng, Z., Zhao, G., et al. (2025) · Oncogene · doi:10.1038/s41388-025-03466-1 · Cited by 1
“However, the broad action of these inhibitors can lead to off-target effects, which may compromise treatment ef fi cacy and increase the risk of adverse effects [14].”
Song, J., Ye, L., Ding, W.-Q., Qiao, H., Dai, J., Bai, H., & Zhang, S. (2025) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2025.09.019 · Cited by 3
“Vorinostat demonstrated notable adverse effects in Phase II trials, including fatigue, nausea, diarrhea, anorexia, dysgeusia, thrombocytopenia, and thrombosis 633 — 635 .”
Sang, D. M., Na, I. H., Anh, D. T., Dung, D. T. M., Hang, N. T. T., Phuong‐Anh, N. T., Pham‐The, H., Oanh, D. T. K., Tùng, T. T., Lee, S. J., et al. (2023) · Chemistry & Biodiversity · doi:10.1002/cbdv.202201030 · Cited by 1
FLIP(L) determines p53 induced life or deathPreprint
Lees, A., McIntyre, A. J., Falcone, F., Crawford, N., McCann, C. K., Quinn, G. P., Roberts, J. Z., Sessler, T., Gallagher, P. F., Gregg, G., et al. (2019) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/858688 · Cited by 1
“HDAC activity is frequently deregulated in cancer, and cancer cells are typically more sensitive to HDAC inhibition than normal cells (Lee et al, 2010); hence, this class of epigenetic modifying enzymes has received significant attention as therapeutic targets, and HDAC inhibitors have achieved several clinical approv…”
BackgroundAbbVie pays $21 billion for Pharmacyclics' BTK inhibitor
Mullard, A. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4605
Antineoplastic and Immunomodulating Agents (L)
Kleemann, A. (2017) · Ullmann's Encyclopedia of Industrial Chemistry · doi:10.1002/14356007.a05_001.pub3
Antineoplastic and Immunomodulating Agents (L)
Kleemann, A. (2022) · Ullmann's Encyclopedia of Industrial Chemistry · doi:10.1002/14356007.a05_001.pub4
Wang, Q., Qiu, H., Zhu, R., Li, R., Qiao, J., Fu, C., Tang, Y., Shen, A., Yan, J., Zhao, D., et al. (2026) · BMC Cancer · doi:10.1186/s12885-026-15816-7
“However, their efficacy against solid tumors remains limited [20, 23–30].”
Non-genetic regulation of chemopersistence in Triple Negative Breast Cancers
Baudre, L. (2024) · theses.fr (ABES) · doi:10.70675/6422f0bbza832z4dcfza920zaa55605f8a31
Pojani, E., Bozo, S., & Mehmeti, I. (2022) · Albanian Journal of Natural and Technical Sciences · doi:10.67537/ajnts2701013
Epigenetic-targeted nanomedicine in cancer: from molecular mechanisms to therapeutic revolution
Wang, B., Han, Y., Zhang, X., Li, Y., Cai, Z., Duan, Z., Gong, Q. H., Jiang, Y., & Luo, K. (2026) · Progress in Materials Science · doi:10.1016/j.pmatsci.2026.101789
Toward Tumor-Conditional Release of Histone Deacetylase Inhibitors from Nongenotoxic Drug Conjugates
Muir, R. K., Gonciarz, R. L., Steri, V., Blank, B. R., Hahn, B., & Renslo, A. R. (2026) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.6c00312
Metadata
- Authors
- Guha, M.
- Corresponding author
- Guha, Malini
- Venue
- Nature Reviews Drug Discovery
- Published
- 2015-04
- Volume
- 14
- Issue
- 4
- Pages
- 225-226
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- 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
- 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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Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
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