The role of protein methyltransferases as potential novel therapeutic targets in squamous cell carcinoma of the head and neck

Oral Oncol. 2018 Jun:81:100-108. doi: 10.1016/j.oraloncology.2018.04.014. Epub 2018 May 3.

Abstract

Squamous cell carcinoma of the head and neck is a lethal disease with suboptimal survival outcomes and standard therapies with significant comorbidities. Whole exome sequencing data recently revealed an abundance of genetic and expression alterations in a family of enzymes known as protein methyltransferases in a variety of cancer types, including squamous cell carcinoma of the head and neck. These enzymes are mostly known for their chromatin-modifying functions through methylation of various histone substrates, though evidence supports their function also through methylation of non-histone substrates. This review summarizes the current knowledge on the function of protein methyltransferases in squamous cell carcinoma of the head and neck and highlights their promising potential as the next generation of therapeutic targets in this disease.

Keywords: EHMT2; EZH2; NSD1; NSD2; NSD3; PRMT1; PRMT5; Protein methylation; Protein methyltransferase; Squamous cell carcinoma of the head and neck.

Publication types

  • Research Support, N.I.H., Intramural
  • Review

MeSH terms

  • Clinical Trials as Topic
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use
  • Epigenesis, Genetic
  • Head and Neck Neoplasms / drug therapy*
  • Head and Neck Neoplasms / enzymology
  • Humans
  • Methylation
  • Mutation
  • Protein Methyltransferases / antagonists & inhibitors*
  • Protein Methyltransferases / genetics
  • Squamous Cell Carcinoma of Head and Neck / drug therapy*
  • Squamous Cell Carcinoma of Head and Neck / enzymology

Substances

  • Enzyme Inhibitors
  • Protein Methyltransferases