The DOI matches its Crossref record; 117 of the 117 references it cites were found in a registry or an index.
The timeline of epigenetic drug discovery: from reality to dreams
Open accessAbstract
The flexibility of the epigenome has generated an enticing argument to explore its reversion through pharmacological treatments as a strategy to ameliorate disease phenotypes. All three families of epigenetic proteins—readers, writers, and erasers—are druggable targets that can be addressed through small-molecule inhibitors. At present, a few drugs targeting epigenetic enzymes as well as analogues of epigenetic modifications have been introduced into the clinic use (e.g. to treat haematological malignancies), and a wide range of epigenetic-based drugs are undergoing clinical trials. Here, we describe the timeline of epigenetic drug discovery and development beginning with the early design based solely on phenotypic observations to the state-of-the-art rational epigenetic drug discovery using validated targets. Finally, we will highlight some of the major aspects that need further research and discuss the challenges that need to be overcome to implement epigenetic drug discovery into clinical management of human disorders. To turn into reality, researchers from various disciplines (chemists, biologists, clinicians) need to work together to optimise the drug engineering, read-out assays, and clinical trial design.
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Cites
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Epigenetics in hepatocellular carcinoma development and therapy: The tip of the iceberg
Fernández-Barrena, M. G., Arechederra, M., Colyn, L., Berasain, C., & Avila, M. A. (2020) · JHEP Reports · doi:10.1016/j.jhepr.2020.100167 · Cited by 126
PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes
Smalley, J. P., Adams, G. E., Millard, C. J., Song, Y., Norris, J. K. S., Schwabe, J. W. R., Cowley, S. M., & Hodgkinson, J. T. (2020) · Chemical Communications · doi:10.1039/d0cc01485k · Cited by 121
Metadata
- Authors
- Ganesan, A., Arimondo, P. B., Rots, M. G., Jeronimo, C., & Berdasco, M.
- Venue
- Clinical Epigenetics
- Published
- 2019-12
- Volume
- 11
- Issue
- 1
- Pages
- 174-174
- ISSN
- 1868-7075 (ISSN-L)
- 1868-7083
- OpenAlex
- W2991108194
- Cited by
- 341
- References
- 117
- FWCI
- 13.75
- Type
- journal article
- Language
- en
- Open access
- gold
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- Ganesan, A., Arimondo, P. B., Rots, M. G., Jeronimo, C., & Berdasco, M. (2019). The timeline of epigenetic drug discovery: from reality to dreams. Clinical Epigenetics. https://doi.org/10.1186/s13148-019-0776-0
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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