Related Experiment Video

Updated: Nov 3, 2025

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
06:07

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors

Published on: August 5, 2022

2.8K

Biochemical perspectives on targeting KMT2 methyltransferases in cancer

Xiang Zhai1, James E Brownell2

  • 1Mechanistic Biology & Profiling, Discovery Sciences, R&D, AstraZeneca, Waltham, MA 02451, USA.

Trends in Pharmacological Sciences
|June 2, 2021
PubMed

Insights

KMT2 methyltransferases regulate gene transcription and are implicated in cancer. Targeting their catalytic activity offers a promising therapeutic strategy for various cancers.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Research

Background:

  • KMT2 methyltransferases are key regulators of gene transcription via histone methylation.
  • These enzymes function within large protein complexes that influence chromatin interactions.
  • KMT2 family genes are linked to cancer, notably KMT2A translocations in mixed-lineage leukemia (MLL).

Purpose of the Study:

  • To review recent advances in KMT2 enzyme mechanisms.
  • To explore KMT2 regulation on nucleosomes.
  • To provide insights for targeting KMT2 methyltransferase activity therapeutically.

Main Methods:

  • Literature review of KMT2 methyltransferases.
  • Analysis of KMT2 enzyme mechanisms and regulation.
  • Examination of KMT2's role in cancer and therapeutic targeting.

Main Results:

  • KMT2 enzymes regulate gene transcription through histone H3 lysine 4 methylation.
  • Protein complexes modulate KMT2 catalytic activity and chromatin binding.
  • Emerging evidence highlights the importance of KMT2 methyltransferase activity in cancer.

Conclusions:

  • Understanding KMT2 mechanisms and regulation is crucial.
  • Targeting the catalytic domain of KMT2 presents a potential cancer therapy.
  • This review offers mechanistic insights for developing KMT2-targeted therapies.
Keywords:
KMT2MLLcancerenzyme mechanismepigeneticslysine methyltransferase

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