Zebularine: a new drug for epigenetic therapy
Abstract
Regulatory genes are often hypermethylated at their promoter 5' regions and silenced in cancer. Epigenetic therapy with DNA methylation inhibitors have been shown to result in the demethylation and reactivation of these genes. Zebularine is a recently discovered mechanism-based inhibitor of DNA methylation, and has received much attention for its potential in clinical use. Further studies exploring the effectiveness of zebularine in a variety of settings could allow the development of novel therapies for cancer.
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Injecting zebularine into the cerebral ventricles of adult rats for seven days reduced DNA methylation of the BDNF promoter.
“In addition, injecting zebularine into the cerebral ventricles of adult rats for seven days reduced DNA methylation of the BDNF promoter.401”
From Epigenetic regulation in major depression and other stress-related disorders: molecular mechanisms, clinical relevance and therapeutic potential (2023) · cites this paper as [401]
Reduced methylation of the BDNF promoter enabled zebularine to restore BDNF expression, suggesting the potential of zebularine as a therapeutic agent in clinical use.
“The reduced methylation of the promoter enabled this drug regimen to restore BDNF expression, suggesting the potential of zebularine as a therapeutic agent in clinical use.”
From Epigenetic regulation in major depression and other stress-related disorders: molecular mechanisms, clinical relevance and therapeutic potential (2023) · cites this paper as [401]
Cites
Targeted mutation of the DNA methyltransferase gene results in embryonic lethality
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Yuan, M., Yang, B., Rothschild, G., Mann, J. J., Sanford, L. D., Tang, X., Huang, C., Wang, C., & Zhang, W. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01519-z · Cited by 246 · see citing works
“401 The reduced methylation of the promoter enabled this drug regimen to restore BDNF expression, suggesting the potential of zebularine as a therapeutic agent in clinical use.”
BackgroundPharmacology of 5-Aza-2′-deoxycytidine (decitabine)
Momparler, R. L. (2005) · Seminars in Hematology · doi:10.1053/j.seminhematol.2005.05.002 · Cited by 231 · see citing works
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At the frontier of epigenetics of brain sex differences
McCarthy, M. M., & Nugent, B. M. (2015) · Frontiers in Behavioral Neuroscience · doi:10.3389/fnbeh.2015.00221 · Cited by 123 · see citing works
Histone modifications, DNA methylation, and Schizophrenia
Gavin, D. P., & Sharma, R. P. (2010) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2009.10.010 · Cited by 121 · see citing works
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- Authors
- Yoo, C. B., Cheng, J. C., & Jones, P. A.
- Affiliations
- University of Southern California (US)
- ORCID
- Jones, P.A.
- Venue
- Biochemical Society Transactions
- Publisher
- Portland Press Ltd.
- Published
- 2004-10-26
- Volume
- 32
- Issue
- 6
- Pages
- 910-912
- ISSN
- 0300-5127 (ISSN-L)
- 1470-8752
- OpenAlex
- W2099166288
- Cited by
- 191
- References
- 1
- Citations by year
- 2026: 4 · 2025: 7 · 2024: 8 · 2023: 9 · 2022: 5 · 2021: 8 · 2020: 7 · 2019: 8 · 2018: 3 · 2017: 7 · 2016: 5 · 2015: 10 · 2014: 11 · 2013: 17 · 2012: 8
- FWCI
- 0.76
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Biochemical Society Transactions (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Biochemical and Molecular Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA modifications and cancer
- Keywords
- zebularine, DNA methylation inhibitors, epigenetic therapy, promoter hypermethylation, demethylation, cancer therapy
- MeSH terms
- Azacitidine, Cytidine, Humans, Neoplasms, Pyrimidine Nucleosides, Genetic Therapy, DNA Methylation, Epigenesis, Genetic
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