The emerging role of KDM5A in human cancer

Guan Jun Yang; Ming Hui Zhu; Xin Jiang Lu; Yan Jun Liu; Jian Fei Lu; Chung Hang Leung; Edmond Dik Lung Ma; Jiong Chen

doi:10.1186/s13045-021-01041-1

The emerging role of KDM5A in human cancer

Guan Jun Yang, Ming Hui Zhu, Xin Jiang Lu, Yan Jun Liu, Jian Fei Lu, Chung Hang Leung^*, Edmond Dik Lung Ma^*, Jiong Chen^*

^*Corresponding author for this work

Department of Chemistry

Research output: Contribution to journal › Review article › peer-review

68 Citations (Scopus)

Abstract

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.

Original language	English
Article number	30
Number of pages	18
Journal	Journal of Hematology and Oncology
Volume	14
Issue number	1
DOIs	https://doi.org/10.1186/s13045-021-01041-1
Publication status	Published - 17 Feb 2021

Scopus Subject Areas

Molecular Biology
Hematology
Oncology
Cancer Research

User-Defined Keywords

Cancer
Drug resistance
Histone methylation
Jumonji C domain
KDM5A
Targeted therapy

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1186/s13045-021-01041-1

Cite this

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title = "The emerging role of KDM5A in human cancer",

abstract = "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.",

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note = "Funding Information: This work is supported by the Natural Science Foundation of Zhejiang Province (LZ18C190001), Hong Kong Baptist University (FRG2/17-18/003), the Health and Medical Research Fund (HMRF/14150561), National Natural Science Foundation of China (22077109 and 21775131), Hong Kong Baptist university Century Club Sponsorship Scheme 2020, Interdisciplinary Research Matching Scheme (RC-IRMS/15-16/03), the Science and Technology Development Fund, Macao SAR (0072/2020/A2), the University of Macau (MYRG2019-00002-ICMS). ",

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AU - Leung, Chung Hang

AU - Ma, Edmond Dik Lung

AU - Chen, Jiong

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N2 - 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.

AB - 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.

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The emerging role of KDM5A in human cancer

Abstract

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