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Published on: February 6, 2015
Epigenetic Therapies and Potential Drugs for Treating Human Cancer
Shi-Qi Lin1, Xia Li1
1College of Marine Science, Shandong University, Weihai 264209, China.
Abstract:
Epigenetic modifications ensure the maintenance of normal cellular functions, and their dysregulation is frequently found in many disease states, including cancer. Nowadays, the most studied epigenetic dysregulation associated with tumorigenesis, cancer progression and metastasis refers to the variations in DNA methylation, histone modification and chromatin structure. The development of novel agents targeting these processes has enabled us to open up new pathways for anti-cancer strategies. To date, many small molecules have been designed to target epigenetic modifiers, and some of them are currently in clinical trials for patients with haematologic malignancies and solid tumours. With this in mind, we elaborate on basic information on epigenetic modifications and potential epigenetic therapies for cancer treatment.
Insights
Epigenetic modifications regulate cell function but are often disrupted in cancer. Novel epigenetic therapies targeting DNA methylation and histone modification show promise for treating various cancers.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Epigenetic modifications are crucial for normal cellular functions.
- Dysregulation of epigenetic processes, including DNA methylation and histone modification, is linked to cancer development, progression, and metastasis.
- Aberrations in chromatin structure also contribute to tumorigenesis.
Purpose of the Study:
- To provide fundamental information on epigenetic modifications.
- To explore the potential of epigenetic therapies in cancer treatment.
- To discuss novel agents targeting epigenetic modifiers.
Main Methods:
- Review of current literature on epigenetic modifications in cancer.
- Analysis of small molecules designed to target epigenetic modifiers.
- Overview of epigenetic therapies in clinical trials.
Main Results:
- Epigenetic dysregulation, particularly DNA methylation and histone modification, is a hallmark of cancer.
- Numerous small molecules targeting epigenetic modifiers have been developed.
- Several epigenetic agents are undergoing clinical trials for hematologic malignancies and solid tumors.
Conclusions:
- Epigenetic modifications play a significant role in cancer biology.
- Targeting epigenetic processes offers promising new avenues for anti-cancer strategies.
- Epigenetic therapies represent a developing frontier in cancer treatment.
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