Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials

Area of Science:

• Molecular Biology
• Oncology
• Pharmacology

Background:

• Epigenetic alterations involve heritable, reversible changes in histone or DNA modifications, regulating gene activity without altering the DNA sequence.
• Epigenetic dysregulation is frequently implicated in human diseases, particularly cancer.
• Epigenetic-targeted therapy is emerging as a viable treatment strategy.

Purpose of the Study:

• To review aberrant enzyme functions in DNA methylation, histone acetylation, and histone methylation during tumor progression.
• To highlight the development of drugs and inhibitors targeting epigenetic enzymes for cancer therapy.

Main Methods:

• Literature review of epigenetic mechanisms in cancer.
• Analysis of drug development targeting epigenetic regulators.
• Summary of clinical and preclinical trial data for epigenetic therapies.

Main Results:

• Aberrant functions of key epigenetic enzymes (DNA methyltransferases, histone deacetylases, histone methyltransferases) contribute to tumorigenesis.
• Numerous inhibitors and drugs targeting these enzymes have been developed.
• Epigenetic therapies have shown promise in hematological malignancies and are being explored for solid tumors.

Conclusions:

• Epigenetic enzymes are critical targets for cancer therapy.
• Targeted epigenetic drugs offer a promising avenue for treating various cancers, including solid tumors.
• Further research and clinical trials are warranted to optimize epigenetic therapies.