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Updated: Aug 11, 2026
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
[New therapeutic approaches for solid tumors: histone deacetylase, methyltransferase and proteasome inhibitors]
Jürgen C Becker1, Selma Ugurel, Eva-Bettina Bröcker
1Universitätsklinik Würzburg, Josef-Schneider-Str. 2, D-97080 Würzburg. becker_jc@klinik.uni-wuerzburg.de
Abstract:
Recent results from basic and translational research on tumor genesis and progression establish the basis for future therapeutic approaches. Targeted therapeutics are tailored toward the molecular abnormalities that cause tumor progression and could potentially provide an effective, non-toxic therapeutic approach in a broad range of cancers including melanoma. Cancer is as much a (cyto)genetic disease as it is an epigenetic disease. Indeed, the fate of the cell depends on a delicate balance between expression and repression of genes. The notion that drastic changes in DNA methylation and histone modifications are present in a variety of human tumors has prompted the development and characterization of epigenetic drugs. Inhibitors of histone deacetylases and methyltransferases as well as of the proteasome are covered in this review.
Insights
This review covers epigenetic drugs, including histone deacetylase and methyltransferase inhibitors, for cancer therapy. These targeted therapeutics address genetic and epigenetic changes driving tumor progression, offering potential non-toxic treatment options.
Area of Science:
- Oncology
- Molecular Biology
- Epigenetics
Context:
- Tumorigenesis and progression are driven by genetic and epigenetic alterations.
- Epigenetic modifications, such as DNA methylation and histone changes, are crucial in cancer development.
- Targeted therapies aim to correct molecular abnormalities underlying cancer progression.
Purpose:
- To review the development and characterization of epigenetic drugs.
- To discuss therapeutic approaches targeting epigenetic dysregulation in various cancers, including melanoma.
- To highlight the potential of epigenetic drugs as effective, non-toxic cancer treatments.
Summary:
- Epigenetic drugs, including inhibitors of histone deacetylases, methyltransferases, and the proteasome, are emerging as promising cancer therapeutics.
- These drugs target the epigenetic landscape of cancer cells, addressing critical gene expression and repression imbalances.
- The review emphasizes the role of epigenetics in cancer, alongside genetics, and the potential of these novel agents in treating diverse malignancies.
Impact:
- Advances in understanding tumor genesis and progression inform future therapeutic strategies.
- Epigenetic therapies offer a new avenue for treating cancers, potentially with reduced toxicity compared to traditional chemotherapy.
- Targeted approaches based on molecular abnormalities hold promise for effective cancer management, including difficult-to-treat cancers like melanoma.
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