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KDM7 Demethylases: Regulation, Function and Therapeutic Targeting
Peng Shao1, Qi Liu1, Hank Heng Qi2
1Department of Anatomy and Cell Biology, Carver College of Medicine, University of Iowa, 51 Newton Road, Iowa City, IA, 52242, USA.
Advances in Experimental Medicine and Biology
|September 26, 2023
Summary
The KDM7 family of histone demethylases, including PHF8 and KDM7A, are crucial regulators in development and cancer. Their diverse demethylation activities and regulatory mechanisms offer potential as therapeutic targets.
Area of Science:
- Biochemistry
- Molecular Biology
- Epigenetics
Background:
- The KDM7 family, comprising PHF8, KDM7A (JHDM1D), and PHF2, was identified over a decade ago.
- These proteins function as histone demethylases, impacting gene transcription, development, and diseases like cancer.
- Growing research elucidates their roles in regulating cell cycle, viability, and migration.
Purpose of the Study:
- To provide a comprehensive overview of the KDM7 family's regulation and functions.
- To discuss the potential of KDM7 family members as therapeutic targets in cancer.
- To highlight future research perspectives for this protein family.
Main Methods:
- Review of existing literature on KDM7 family members.
- Analysis of demethylation activities on various histone marks (e.g., H3K9me2/1, H3K27me2, H4K20me1/3).
- Examination of post-transcriptional and post-translational regulations.
Main Results:
- PHF8 and KDM7A demethylate H3K9me2/1, H3K27me2, and H4K20me1.
- PHF2 demethylates H3K9me2 (PKA-dependent) and uniquely H4K20me3.
- PHF8 plays significant roles in cell cycle, viability, and migration, implicating it in oncogenesis.
Conclusions:
- The KDM7 family exhibits diverse demethylase activities and regulatory pathways.
- Understanding these epigenetic regulators is crucial for cancer therapy development.
- Further investigation into KDM7 family functions and regulation is warranted.
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