Druggability of the enzymes of the non-mevalonate-pathway

Drug Discov Today. 2013 Dec;18(23-24):1256-62. doi: 10.1016/j.drudis.2013.07.003. Epub 2013 Jul 13.

Abstract

The non-mevalonate pathway constitutes a source of novel drug targets. This biosynthetic route is essential for pathogens but is absent in humans. Our systematic evaluation of the druggability of all enzymes provides a convenient way of selecting targets that should be most easily inhibited by small-molecule drugs. We found that not every target is equally druggable and we identified novel, druggable, potentially allosteric sites. These results should accelerate the development of anti-infective drugs with a novel mode of action, which are needed ever more urgently in light of the rapid emergence of drug-resistant strains.

Publication types

  • Review

MeSH terms

  • Allosteric Site
  • Anti-Infective Agents / pharmacology*
  • Biosynthetic Pathways / drug effects
  • Drug Design*
  • Drug Resistance, Microbial
  • Enzyme Inhibitors / pharmacology
  • Enzymes / drug effects
  • Enzymes / metabolism
  • Humans
  • Mevalonic Acid / metabolism
  • Molecular Targeted Therapy*

Substances

  • Anti-Infective Agents
  • Enzyme Inhibitors
  • Enzymes
  • Mevalonic Acid