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Targeting histone demethylase KDM5B for cancer treatment

Yun-Dong Fu1, Ming-Jie Huang1, Jia-Wen Guo1

  • 1Green Catalysis Center, And College of Chemistry, Zhengzhou University, Zhengzhou, 450001, China.

European Journal of Medicinal Chemistry
|September 5, 2020
PubMed

Insights

Lysine-Specific Demethylase 5B (KDM5B) is an oncogene driving cancer. This review details KDM5B

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Research

Background:

  • Lysine-Specific Demethylase 5B (KDM5B) regulates chromatin structure by demethylating H3K4me2/3, impacting gene transcription.
  • KDM5B acts as an oncogene, closely associated with the progression of human cancers.
  • Targeting KDM5B presents a promising therapeutic strategy for cancer treatment, notably with inhibitors like CPI-455.

Purpose of the Study:

  • To provide a comprehensive overview of Lysine-Specific Demethylase 5B (KDM5B).
  • To summarize the progress in understanding KDM5B's structure, function, and role in cancer.
  • To review the development and structure-activity relationship (SAR) studies of KDM5B inhibitors.

Main Methods:

  • Literature review of KDM5B research.
  • Analysis of crystal structures and biochemical screening data for KDM5B inhibitors.
  • Summary of structure-activity relationship (SAR) studies for KDM5B inhibitors.

Main Results:

  • KDM5B's role in transcriptional repression and chromatin regulation is detailed.
  • The association of KDM5B with various human cancers is highlighted.
  • Current KDM5B inhibitors, primarily Fe(II) chelators, and their mechanisms are discussed.

Conclusions:

  • KDM5B is a significant oncogene and a viable therapeutic target in cancer.
  • Understanding KDM5B's structure and inhibition mechanisms is crucial for drug development.
  • This review consolidates current knowledge on KDM5B and its inhibitors, guiding future research.
Keywords:
CancerFe(2+)InhibitorsKDM5BTranscriptional repression

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