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Small Molecules Targeting HATs, HDACs, and BRDs in Cancer Therapy
Donglu Wu1,2, Ye Qiu2,3, Yunshuang Jiao3
1School of Clinical Medical, Changchun University of Chinese Medicine, Changchun, China.
Abstract:
Evidence for research over the past decade shows that epigenetic regulation mechanisms run through the development and prognosis of tumors. Therefore, small molecular compounds targeting epigenetic regulation have become a research hotspot in the development of cancer therapeutic drugs. According to the obvious abnormality of histone acetylation when tumors occur, it suggests that histone acetylation modification plays an important role in the process of tumorigenesis. Currently, as a new potential anti-cancer therapeutic drugs, many active small molecules that target histone acetylation regulatory enzymes or proteins such as histone deacetylases (HDACs), histone acetyltransferase (HATs) and bromodomains (BRDs) have been developed to restore abnormal histone acetylation levels to normal. In this review, we will focus on summarizing the changes of histone acetylation levels during tumorigenesis, as well as the possible pharmacological mechanisms of small molecules that target histone acetylation in cancer treatment.
Insights
Small molecules targeting epigenetic regulation, specifically histone acetylation, show promise as cancer therapeutics. These drugs aim to restore normal histone acetylation levels crucial for preventing and treating tumors.
Area of Science:
- Molecular Biology
- Oncology
- Epigenetics
Background:
- Epigenetic regulation is increasingly recognized for its role in tumor development and prognosis.
- Abnormal histone acetylation is a hallmark of cancer, indicating its significance in tumorigenesis.
- Targeting epigenetic mechanisms represents a promising strategy for novel cancer therapeutics.
Purpose of the Study:
- To review the alterations in histone acetylation levels during cancer development.
- To summarize the pharmacological mechanisms of small molecules targeting histone acetylation for cancer treatment.
- To highlight the potential of targeting histone acetylation regulatory enzymes and proteins in oncology.
Main Methods:
- Review of recent scientific literature on epigenetic regulation in cancer.
- Analysis of studies focusing on small molecules targeting histone acetylation.
- Examination of enzymes and proteins involved in histone acetylation, including HDACs, HATs, and BRDs.
Main Results:
- Significant changes in histone acetylation patterns are observed during tumorigenesis.
- Development of various small molecules targeting key regulators of histone acetylation.
- These molecules aim to normalize aberrant histone acetylation levels in cancer cells.
Conclusions:
- Targeting histone acetylation is a viable strategy for developing new anti-cancer drugs.
- Small molecules modulating histone acetylation offer potential therapeutic benefits in cancer treatment.
- Further research into these epigenetic modulators could lead to improved cancer therapies.
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