Related Experiment Video
Updated: Jun 28, 2025
Author Spotlight: Epigenetic Modifications and Metabolic Rewiring as Targets for Cancer Therapy
Published on: October 18, 2024
Deciphering the interplay of histone post-translational modifications in cancer: Co-targeting histone modulators for
Rawan R Kawaf1, Wafaa S Ramadan2, Raafat El-Awady1
1College of Pharmacy, University of Sharjah, Sharjah 27272, United Arab Emirates; Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates.
Abstract:
Chromatin undergoes dynamic regulation through reversible histone post-translational modifications (PTMs), orchestrated by "writers," "erasers," and "readers" enzymes. Dysregulation of these histone modulators is well implicated in shaping the cancer epigenome and providing avenues for precision therapies. The approval of six drugs for cancer therapy targeting histone modulators, along with the ongoing clinical trials of numerous candidates, represents a significant advancement in the field of precision medicine. Recently, it became apparent that histone PTMs act together in a coordinated manner to control gene expression. The intricate crosstalk of histone PTMs has been reported to be dysregulated in cancer, thus emerging as a critical factor in the complex landscape of cancer development. This formed the foundation of the swift emergence of co-targeting different histone modulators as a new strategy in cancer therapy. This review dissects how histone PTMs, encompassing acetylation, phosphorylation, methylation, SUMOylation and ubiquitination, collaboratively influence the chromatin states and impact cellular processes. Furthermore, we explore the significance of histone modification crosstalk in cancer and discuss the potential of targeting histone modification crosstalk in cancer management. Moreover, we underscore the significant strides made in developing dual epigenetic inhibitors, which hold promise as emerging candidates for effective cancer therapy.
Insights
Histone post-translational modifications (PTMs) coordinate gene expression, and their crosstalk is crucial in cancer development. Targeting this crosstalk with dual epigenetic inhibitors offers a promising new strategy for cancer therapy.
Area of Science:
- Epigenetics and Molecular Biology
- Cancer Research
Background:
- Histone post-translational modifications (PTMs) dynamically regulate chromatin and gene expression.
- Dysregulation of histone modulators is linked to cancer epigenome alterations.
- Coordinated action of histone PTMs is increasingly recognized in controlling cellular processes.
Purpose of the Study:
- To review the collaborative influence of histone PTMs on chromatin states and cellular functions.
- To explore the significance of histone modification crosstalk in cancer development.
- To discuss the therapeutic potential of targeting histone modification crosstalk in cancer management.
Main Methods:
- Literature review focusing on histone PTMs (acetylation, phosphorylation, methylation, SUMOylation, ubiquitination).
- Analysis of the role of histone modification crosstalk in cancer.
- Exploration of dual epigenetic inhibitors for cancer therapy.
Main Results:
- Histone PTMs, including acetylation, phosphorylation, methylation, SUMOylation, and ubiquitination, work together to regulate chromatin.
- Histone modification crosstalk is dysregulated in cancer, contributing to its development.
- Dual epigenetic inhibitors targeting multiple histone modulators show promise in preclinical and clinical studies.
Conclusions:
- Targeting the crosstalk between histone PTMs represents a novel therapeutic strategy for cancer.
- Dual epigenetic inhibitors offer a promising avenue for precision cancer therapy by modulating coordinated histone modifications.
- Further research into histone modification crosstalk could unveil new targets and improve cancer treatment outcomes.
More Related Videos
10:41An Integrated Platform for Genome-wide Mapping of Chromatin States Using High-throughput ChIP-sequencing in Tumor Tissues
Published on: April 5, 2018
08:12Global Level Quantification of Histone Post-Translational Modifications in a 3D Cell Culture Model of Hepatic Tissue
Published on: May 5, 2022
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
02:32Histone Modification
02:04Covalently Linked Protein Regulators
These groups modify specific amino acids in a protein....
02:50Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
02:25Spreading of Chromatin Modifications
Writers
The writer...
01:37Epigenetic Regulation
X-chromosome...