Current topics on inhibitors of respiratory complex I

Biochim Biophys Acta. 2016 Jul;1857(7):884-91. doi: 10.1016/j.bbabio.2015.11.009. Epub 2015 Nov 26.


There are a variety of chemicals which regulate the functions of bacterial and mitochondrial complex I. Some of them, such as rotenone and piericidin A, have been indispensable molecular tools in mechanistic studies on complex I. A large amount of experimental data characterizing the actions of complex I inhibitors has been accumulated so far. Recent X-ray crystallographic structural models of entire complex I may be helpful to carefully interpret this data. We herein focused on recent hot topics on complex I inhibitors and the subjects closely connected to these inhibitors, which may provide useful information not only on the structural and functional aspects of complex I, but also on drug design targeting this enzyme. This article is part of a Special Issue entitled Respiratory complex I, edited by Volker Zickermann and Ulrich Brandt.

Keywords: Chemical modifications of protein; Complex I; Inhibitors.

Publication types

  • Review

MeSH terms

  • Binding Sites
  • Drug Design*
  • Electron Transport Complex I / antagonists & inhibitors*
  • Electron Transport Complex I / ultrastructure*
  • Enzyme Activation / drug effects
  • Enzyme Inhibitors / chemistry*
  • Models, Chemical*
  • Models, Molecular*
  • Protein Binding
  • Protein Conformation
  • Structure-Activity Relationship


  • Enzyme Inhibitors
  • Electron Transport Complex I