Research progress of dual inhibitors targeting crosstalk between histone epigenetic modulators for cancer therapy

Area of Science:

• Oncology
• Epigenetics
• Pharmacology

Background:

• Abnormal epigenetics is a key feature of human cancers.
• Histone epigenetic modulators are promising anticancer drug targets, with approved therapies and ongoing clinical trials.
• Current single-target epigenetic inhibitors face challenges including limited efficacy, resistance, and toxicity.

Purpose of the Study:

• To review the intricate crosstalk of histone epigenetic modulators in gene transcription.
• To summarize the progress of dual epigenetic inhibitors targeting this crosstalk.
• To highlight a strategy for overcoming limitations of single-target epigenetic drugs.

Main Methods:

• Literature review of histone epigenetic modulators.
• Analysis of cooperative mechanisms in epigenetic regulation.
• Summary of dual epigenetic inhibitor development and targeting strategies.

Main Results:

• Histone epigenetic modulators exhibit complex crosstalk influencing gene transcription.
• Co-targeting these modulators offers a promising strategy to enhance therapeutic profiles.
• Dual epigenetic inhibitors are emerging to address limitations of single-target approaches.

Conclusions:

• Understanding crosstalk is crucial for effective epigenetic cancer therapy.
• Dual epigenetic inhibitors represent a significant advancement in overcoming drug resistance and toxicity.
• Targeting histone epigenetic modulator crosstalk holds potential for improved cancer treatment outcomes.