Pharmacological inhibition of KDM5A for cancer treatment

Guan Jun Yang, Jia Wu, Liang Miao, Ming Hui Zhu, Qian Jin Zhou, Xin Jiang Lu, Jian Fei Lu, Chung-Hang Leung*, Dik Lung Ma*, Jiong Chen*

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

20 Citations (Scopus)


Lysine-specific demethylase 5A (KDM5A, also named RBP2 or JARID1A) is a demethylase that can remove methyl groups from histones H3K4me1/2/3. It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, drug resistance, and is associated with poor prognosis. Pharmacological inhibition of KDM5A has been reported to significantly attenuate tumor progression in vitro and in vivo in a range of solid tumors and acute myeloid leukemia. This review will present the structural aspects of KDM5A, its role in carcinogenesis, a comparison of currently available approaches for screening KDM5A inhibitors, a classification of KDM5A inhibitors, and its potential as a drug target in cancer therapy.

Original languageEnglish
Article number113855
JournalEuropean Journal of Medicinal Chemistry
Publication statusPublished - 15 Dec 2021

Scopus Subject Areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

User-Defined Keywords

  • Cancer therapy
  • Drug resistance
  • Histone methylation
  • Lysine-specific demethylase 5A
  • Screening methods


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