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Updated: Feb 22, 2026

An Integrated Platform for Genome-wide Mapping of Chromatin States Using High-throughput ChIP-sequencing in Tumor Tissues
Published on: April 5, 2018
Molecular Mechanisms of Epigenetic Regulators as Activatable Targets in Cancer Theranostics
Yinglu Li1,2, Zhiming Li1,2, Wei-Guo Zhu1,2
1Shenzhen University School of Medicine, Shenzhen 518060, China.
Abstract:
Epigenetics is defined as somatically inheritable changes that are not accompanied by alterations in DNA sequence. Epigenetics encompasses DNA methylation, covalent histone modifications, non-coding RNA as well as nucleosome remodeling. Notably, abnormal epigenetic changes play a critical role in cancer development including malignant transformation, metastasis, prognosis, drug resistance and tumor recurrence, which can provide effective targets for cancer prognosis, diagnosis and therapy. Understanding these changes provide effective means for cancer diagnosis and druggable targets for better clinical applications. Histone modifications and related enzymes have been found to correlate well with cancer incidence and prognosis in recent years. Dysregulated expression or mutation of histone modification enzymes and histone modification status abnormalities have been considered to play essential roles in tumorigenesis and clinical outcomes of cancer treatment. Some of the histone modification inhibitors have been extensively employed in clinical practice and many others are still under laboratory research or pre-clinical assessment. Here we summarize the important roles of epigenetics, especially histone modifications in cancer diagnostics and therapeutics, and also discuss the developmental implications of activatable epigenetic targets in cancer theranostics.
Insights
Epigenetics, inheritable changes without DNA alteration, is crucial in cancer. Understanding epigenetic modifications, especially histone modifications, offers new diagnostic and therapeutic strategies for cancer.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Epigenetics involves heritable changes in gene expression without altering DNA sequence, including DNA methylation and histone modifications.
- Aberrant epigenetic alterations are key drivers in cancer development, influencing malignant transformation, metastasis, and drug resistance.
Purpose of the Study:
- To summarize the critical roles of epigenetics, particularly histone modifications, in cancer diagnostics and therapeutics.
- To discuss the implications of activatable epigenetic targets for cancer theranostics.
Main Methods:
- Review of current literature on epigenetics and histone modifications in cancer.
- Analysis of the role of histone modification enzymes and their inhibitors in tumorigenesis and treatment.
Main Results:
- Abnormal epigenetic changes are integral to cancer progression and recurrence.
- Histone modifications and associated enzymes are linked to cancer incidence and patient prognosis.
- Several histone modification inhibitors are in clinical use or under investigation.
Conclusions:
- Epigenetic insights, especially regarding histone modifications, provide valuable targets for cancer diagnosis and therapy.
- Activatable epigenetic targets hold promise for advancing cancer theranostics.
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