The emerging role of KDM5A in human cancer

Histone methylation is a key posttranslational modification of chromatin, and its dysregulation affects a wide array of nuclear activities including the maintenance of genome integrity, transcriptional regulation, and epigenetic inheritance. Variations in the pattern of histone methylation influence...

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Bibliographic Details
Published in:Journal of hematology and oncology 2021-02, Vol.14 (1), p.30-30, Article 30
Main Authors: Yang, Guan-Jun, Zhu, Ming-Hui, Lu, Xin-Jiang, Liu, Yan-Jun, Lu, Jian-Fei, Leung, Chung-Hang, Ma, Dik-Lung, Chen, Jiong
Format: Article
Language:English
Subjects:
Antitumor activity
Breast cancer
Cancer
Cell cycle
Cell growth
Chromatin
Disease
Drug resistance
Epigenetic inheritance
Epigenetics
Gene regulation
Genes
Genetic aspects
Genetic transcription
Genomes
Hematology
Heredity
Histone H3
Histone methylation
Histones
Homeostasis
Jumonji C domain
KDM5A
Leukemia
Lung cancer
Lysine
Metastasis
Methylation
Motility
Oncology
Oncology, Experimental
Pediatrics
Physiological aspects
Post-translational modification
Prostate
Proteins
Review
Senescence
Stem cells
Targeted therapy
Transcription
Transcription factors
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Summary:Histone methylation is a key posttranslational modification of chromatin, and its dysregulation affects a wide array of nuclear activities including the maintenance of genome integrity, transcriptional regulation, and epigenetic inheritance. Variations in the pattern of histone methylation influence both physiological and pathological events. Lysine-specific demethylase 5A (KDM5A, also known as JARID1A or RBP2) is a KDM5 Jumonji histone demethylase subfamily member that erases di- and tri-methyl groups from lysine 4 of histone H3. Emerging studies indicate that KDM5A is responsible for driving multiple human diseases, particularly cancers. In this review, we summarize the roles of KDM5A in human cancers, survey the field of KDM5A inhibitors including their anticancer activity and modes of action, and the current challenges and potential opportunities of this field.
ISSN:1756-8722
1756-8722
DOI:10.1186/s13045-021-01041-1