The emerging role of KDM5A in human cancer

Journal of Hematology & Oncology

Dik-Lung Ma¹  Yan-Jun Liu²  Chung-Hang Leung³  Jiong Chen⁴  Ming-Hui Zhu⁴  Jian-Fei Lu⁴  Xin-Jiang Lu⁴  Guan-Jun Yang⁵ 

[1] Department of Chemistry, Hong Kong Baptist University, 999077, Kowloon, Hong Kong, People’s Republic of China;Department of Immunology and Medical Microbiology, Nanjing University of Chinese Medicine, 210046, Nanjing, People’s Republic of China;Institute of Chinese Medical Sciences, State Key Laboratory of Quality Research in Chinese Medicine, University of Macau, Macao SAR, People’s Republic of China;State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-Products, Ningbo University, 315211, Ningbo, Zhejiang, People’s Republic of China;Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, 315211, Ningbo, People’s Republic of China;Key Laboratory of Applied Marine Biotechnology of Ministry of Education, Ningbo University, 315211, Ningbo, People’s Republic of China;State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-Products, Ningbo University, 315211, Ningbo, Zhejiang, People’s Republic of China;Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, 315211, Ningbo, People’s Republic of China;Key Laboratory of Applied Marine Biotechnology of Ministry of Education, Ningbo University, 315211, Ningbo, People’s Republic of China;Institute of Chinese Medical Sciences, State Key Laboratory of Quality Research in Chinese Medicine, University of Macau, Macao SAR, People’s Republic of China;

关键词: KDM5A;    Cancer;    Jumonji C domain;    Histone methylation;    Drug resistance;    Targeted therapy;   

DOI  :  10.1186/s13045-021-01041-1

来源: Springer

【 摘 要 】

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.

【 授权许可】

CC BY