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Updated: Apr 28, 2026
Biochemical Assays for Analyzing Activities of ATP-dependent Chromatin Remodeling Enzymes
Published on: October 25, 2014
ATP-dependent chromatin remodeling complexes as novel targets for cancer therapy
Kimberly Mayes1, Zhijun Qiu1, Aiman Alhazmi1
1Department of Human and Molecular Genetics, VCU Institute of Molecular Medicine, Massey Cancer Center, Virginia Commonwealth University School of Medicine, Richmond, Virginia, USA.
Abstract:
The progression to advanced stage cancer requires changes in many characteristics of a cell. These changes are usually initiated through spontaneous mutation. As a result of these mutations, gene expression is almost invariably altered allowing the cell to acquire tumor-promoting characteristics. These abnormal gene expression patterns are in part enabled by the posttranslational modification and remodeling of nucleosomes in chromatin. These chromatin modifications are established by a functionally diverse family of enzymes including histone and DNA-modifying complexes, histone deposition pathways, and chromatin remodeling complexes. Because the modifications these enzymes deposit are essential for maintaining tumor-promoting gene expression, they have recently attracted much interest as novel therapeutic targets. One class of enzyme that has not generated much interest is the chromatin remodeling complexes. In this review, we will present evidence from the literature that these enzymes have both causal and enabling roles in the transition to advanced stage cancers; as such, they should be seriously considered as high-value therapeutic targets. Previously published strategies for discovering small molecule regulators to these complexes are described. We close with thoughts on future research, the field should perform to further develop this potentially novel class of therapeutic target.
Insights
Chromatin remodeling complexes play key roles in cancer progression by altering gene expression. Targeting these enzymes offers a promising new therapeutic strategy for advanced stage cancers.
Area of Science:
- Molecular Biology
- Cancer Biology
- Epigenetics
Background:
- Cancer progression involves cellular changes initiated by mutations, leading to altered gene expression.
- Abnormal gene expression patterns in cancer are influenced by chromatin modifications.
- Histone and DNA-modifying complexes, histone deposition pathways, and chromatin remodeling complexes establish these modifications.
Purpose of the Study:
- To review the literature on the role of chromatin remodeling complexes in cancer.
- To highlight chromatin remodeling complexes as potential therapeutic targets.
- To discuss strategies for discovering small molecule regulators of these complexes.
Main Methods:
- Literature review of existing research on chromatin remodeling complexes in cancer.
- Analysis of the functional roles of these enzymes in tumor promotion.
- Examination of previously published strategies for small molecule regulator discovery.
Main Results:
- Chromatin remodeling complexes have both causal and enabling roles in the transition to advanced stage cancers.
- These enzymes are essential for maintaining tumor-promoting gene expression.
- Chromatin remodeling complexes represent high-value therapeutic targets.
Conclusions:
- Chromatin remodeling complexes should be seriously considered as novel therapeutic targets for cancer.
- Further research is needed to develop small molecule regulators for these complexes.
- Targeting chromatin remodeling complexes holds potential for treating advanced stage cancers.
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