m6A RNA methylation and beyond - The epigenetic machinery and potential treatment options

Drug Discov Today. 2021 Nov;26(11):2559-2574. doi: 10.1016/j.drudis.2021.06.004. Epub 2021 Jun 12.

Abstract

m6A is emerging as one of the most important RNA modifications because of its involvement in pathological and physiological events. Here, we provide an overview of this epitranscriptomic modification, beginning with a description of the molecular players involved and continuing with a focus on the role of m6A in the maintenance of stemness, induction of the epithelial to mesenchymal transition (EMT), and tumor progression. Finally, we discuss the state of the art regarding the design and validation of inhibitors of m6A writers or erasers to provide a background for future investigations and for the development of specific therapeutics.

Keywords: Cancer; Epitranscriptomics; METTL3; RNA; m6A.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Epigenesis, Genetic
  • Epigenomics
  • Epithelial-Mesenchymal Transition / genetics*
  • Gene Expression Profiling
  • Gene Expression Regulation / genetics*
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Methylation
  • Methyltransferases / antagonists & inhibitors*
  • Neoplasms / drug therapy
  • Neoplasms / genetics*
  • RNA Processing, Post-Transcriptional / genetics*
  • Stem Cells / metabolism*

Substances

  • 6-methyladenine mRNA methyltransferase
  • Methyltransferases