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Targeting histone demethylases as a potential cancer therapy (Review)
Wenfei Diao1, Jiabin Zheng1, Yong Li1
1Department of Gastrointestinal Surgery, Department of General Surgery, Guangdong Provincial People's Hospital, Guangdong Academy of Medical Sciences, Guangzhou, Guangdong 510080, P.R. China.
Abstract:
Post‑translational modifications of histones by histone demethylases have an important role in the regulation of gene transcription and are implicated in cancers. Recently, the family of lysine (K)‑specific demethylase (KDM) proteins, referring to histone demethylases that dynamically regulate histone methylation, were indicated to be involved in various pathways related to cancer development. To date, numerous studies have been conducted to explore the effects of KDMs on cancer growth, metastasis and drug resistance, and a majority of KDMs have been indicated to be oncogenes in both leukemia and solid tumors. In addition, certain KDM inhibitors have been developed and have become the subject of clinical trials to explore their safety and efficacy in cancer therapy. However, most of them focus on hematopoietic malignancy. This review summarizes the effects of KDMs on tumor growth, drug resistance and the current status of KDM inhibitors in clinical trials.
Insights
Lysine (K)-specific demethylase (KDM) proteins regulate gene transcription and are implicated in cancer. This review summarizes KDM roles in tumor growth, drug resistance, and clinical trials of KDM inhibitors.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Post-translational modifications of histones, particularly histone methylation, are crucial for gene transcription regulation.
- Histone demethylases, specifically lysine (K)-specific demethylase (KDM) proteins, dynamically regulate histone methylation.
- KDMs are increasingly implicated in diverse cancer development pathways.
Purpose of the Study:
- To review the multifaceted roles of KDMs in cancer progression, including tumor growth, metastasis, and drug resistance.
- To provide an overview of the current landscape of KDM inhibitors in clinical development for cancer therapy.
- To highlight the focus of current KDM inhibitor trials, particularly in relation to hematopoietic malignancies.
Main Methods:
- Literature review of studies investigating KDM functions in cancer.
- Analysis of research on the oncogenic roles of various KDMs in leukemia and solid tumors.
- Survey of ongoing and completed clinical trials for KDM inhibitors.
Main Results:
- A majority of KDMs function as oncogenes, promoting cancer growth, metastasis, and drug resistance in various cancers.
- Numerous KDM inhibitors have been developed, with several undergoing clinical trials.
- Current clinical trials predominantly focus on KDM inhibitors for hematopoietic malignancies.
Conclusions:
- KDMs are critical regulators in cancer development and represent promising therapeutic targets.
- KDM inhibitors show potential in cancer treatment, though further research is needed, especially for solid tumors.
- The clinical development of KDM inhibitors is advancing, with ongoing trials evaluating their safety and efficacy.
