Recent developments of small molecules targeting RNA m6A modulators

Eur J Med Chem. 2020 Jun 15:196:112325. doi: 10.1016/j.ejmech.2020.112325. Epub 2020 Apr 15.

Abstract

N6-methyladenosine (m6A) is the most abundant internal post-transcriptional modification in eukaryotic mRNA. The development of emerging technologies such as m6A-seq, has helped reveal the fundamental role of m6A-RNA in regulation of the mammalian transcriptome. With the identification and advances in the understanding of m6A modulators, the relationship between m6A and human diseases is gradually being revealed. This review summarizes recent progress in the understanding of the role of m6A modulators in human disease and their structural characteristics. We highlight the potential of small-molecule regulators targeting m6A associated proteins as tool molecules and disease treatment options from the medicinal chemistry perspective.

Keywords: Epigenetics; N(6)-methyladenosine; Small-molecule regulators.

Publication types

  • Review

MeSH terms

  • Adenine / analogs & derivatives*
  • Adenine / metabolism
  • Animals
  • Humans
  • Models, Molecular
  • Molecular Structure
  • RNA, Messenger / metabolism*
  • Small Molecule Libraries / chemical synthesis
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*

Substances

  • RNA, Messenger
  • Small Molecule Libraries
  • Adenine
  • 6-methyladenine