Protein methyltransferases as a target class for drug discovery

Nat Rev Drug Discov. 2009 Sep;8(9):724-32. doi: 10.1038/nrd2974.


The protein methyltransferases (PMTs) - which methylate protein lysine and arginine residues and have crucial roles in gene transcription - are emerging as an important group of enzymes that play key parts in normal physiology and human diseases. The collection of human PMTs is a large and diverse group of enzymes that have a common mechanism of catalysis. Here, we review the biological, biochemical and structural data that together present PMTs as a novel, chemically tractable target class for drug discovery.

Publication types

  • Review

MeSH terms

  • Catalytic Domain
  • Drug Design
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Genome, Human
  • Humans
  • Models, Molecular
  • Pharmacology / trends
  • Protein Methyltransferases / antagonists & inhibitors*
  • Protein Methyltransferases / genetics
  • Protein Methyltransferases / physiology


  • Enzyme Inhibitors
  • Protein Methyltransferases