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Pharmacological inhibition of KDM5A for cancer treatment

Guan-Jun Yang1, Jia Wu2, Liang Miao1

  • 1State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products, Ningbo University, Ningbo, 315211, Zhejiang, China; Laboratory of Biochemistry and Molecular Biology, School of Marine Sciences, Ningbo University, Ningbo, 315211, China; Key Laboratory of Applied Marine Biotechnology of Ministry of Education, Ningbo University, Ningbo, 315211, China.

European Journal of Medicinal Chemistry
|September 23, 2021
PubMed

Insights

Lysine-specific demethylase 5A (KDM5A) is a cancer-driving enzyme. Inhibiting KDM5A shows promise for treating various cancers by blocking tumor progression.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Lysine-specific demethylase 5A (KDM5A) is a histone demethylase involved in epigenetic regulation.
  • Aberrant KDM5A expression is linked to various cancers, promoting proliferation, metastasis, and drug resistance.
  • KDM5A inhibition has shown potential in attenuating tumor progression in preclinical models.

Purpose of the Study:

  • To review the structural features of KDM5A.
  • To elucidate the role of KDM5A in carcinogenesis.
  • To compare KDM5A inhibitor screening methods and classify existing inhibitors.
  • To assess KDM5A's potential as a cancer drug target.

Main Methods:

  • Literature review of KDM5A structure, function, and inhibitors.
  • Analysis of KDM5A's role in cancer development and progression.
  • Comparison of high-throughput screening assays for KDM5A inhibitors.
  • Classification of KDM5A inhibitors based on their mechanisms.

Main Results:

  • KDM5A's demethylase activity on H3K4me1/2/3 is crucial for its oncogenic functions.
  • KDM5A promotes cancer cell proliferation, metastasis, invasiveness, and drug resistance.
  • Various screening approaches and inhibitor classes targeting KDM5A have been identified.

Conclusions:

  • KDM5A is a validated drug target in oncology.
  • Inhibiting KDM5A offers a therapeutic strategy for solid tumors and acute myeloid leukemia.
  • Further research into KDM5A inhibitors could lead to novel cancer treatments.
Keywords:
Cancer therapyDrug resistanceHistone methylationLysine-specific demethylase 5AScreening methods

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