Multiple functions of the lysine methyltransferase KMT5a in cancer: potential targets for innovative therapies

Related Experiment Video

Updated: Jan 16, 2026

Specificity Analysis of Protein Lysine Methyltransferases Using SPOT Peptide Arrays
08:48

Specificity Analysis of Protein Lysine Methyltransferases Using SPOT Peptide Arrays

Published on: November 29, 2014

14.4K

Rosa Della Monica1, Michela Buonaiuto2,3, Mariella Cuomo2,3

  • 1CEINGE-Advanced Biotechnologies "Franco Salvatore", Via G. Salvatore 486, 80145, Naples, Italy. dellamonica@ceinge.unina.it.

Clinical Epigenetics
|September 30, 2025
PubMed

Insights

Lysine methyltransferase 5a (KMT5a) regulates gene transcription and DNA repair, impacting cancer development. This enzyme

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Lysine methyltransferase 5a (KMT5a) is implicated in human disease pathogenesis.
  • KMT5a's role in cancer development and progression is multifaceted.

Purpose of the Study:

  • To review the diverse impacts of KMT5a activity on human cancer.
  • To highlight KMT5a as a potential therapeutic target.

Main Methods:

  • Review of existing literature on KMT5a function in cancer.
  • Analysis of KMT5a's roles in histone modification, DNA repair, and nonhistone protein methylation.

Main Results:

  • KMT5a specifically monomethylates histone 4 (H4) at lysine 20, affecting chromatin organization and oncogene/tumor suppressor gene transcription.
  • KMT5a influences DNA double-strand break repair pathways, impacting genomic instability.
  • KMT5a methylates nonhistone proteins like TP53, affecting cancer cell functions.
  • KMT5a is overexpressed in various human cancers, exhibiting protumorigenic activity.

Conclusions:

  • KMT5a plays a significant role in cancer development and progression through epigenetic and protein modification mechanisms.
  • KMT5a's overexpression and protumorigenic activity establish it as a promising target for novel cancer therapies.
Keywords:
Cancer evolutionCancer stem cellsCancer therapyDNA repairH4K20Histone methylationKMT5a/PR-Set7/Set8/SETD8Protein methylation

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