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

Research output: Contribution to journalReview articlepeer-review

60 Citations (Scopus)


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 languageEnglish
Article number30
Number of pages18
JournalJournal of Hematology and Oncology
Issue number1
Publication statusPublished - 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


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