Epigenetically Active Drugs Inhibiting DNA Methylation and Histone Deacetylation

Area of Science:

• Molecular Biology
• Cancer Biology
• Epigenetics

Background:

• Epigenetic mechanisms regulate gene expression but disruptions are linked to diseases like cancer.
• Aberrant epigenetic changes in cancer promote stemness, inhibit differentiation, and impair cell cycle control.
• These abnormal epigenetic patterns are potentially reversible by epigenetically active agents.

Purpose of the Study:

• To explore the role of epigenetic alterations in cancer development.
• To investigate the therapeutic potential of epigenetically active agents in cancer treatment.
• To highlight challenges in using epigenetic drugs for solid tumors and advanced cancers.

Main Methods:

• Review of epigenetic machinery, including DNA/histone modifiers and chromatin remodelers.
• Analysis of chemical substances influencing epigenetic factors, such as DNA methyltransferase inhibitors and histone deacetylase inhibitors.
• Examination of preclinical and clinical data on the efficacy of epigenetic drugs in various cancers.

Main Results:

• Epigenetic dysregulation contributes to neoplastic properties in cancer cells.
• Epigenetically active agents demonstrate efficacy in preclinical cancer models.
• Several epigenetic compounds are approved for hematological malignancies.
• Challenges remain for treating non-hematological solid tumors and chemoresistant cancers.

Conclusions:

• Epigenetic drugs represent a promising therapeutic strategy for cancer.
• Targeting epigenetic modifications can reverse aberrant cancer cell phenotypes.
• Further research is needed to overcome limitations for broader clinical application, particularly in solid tumors.