Current topics on inhibitors of respiratory complex I

• Published in: Biochimica et biophysica acta Vol. 1857; no. 7; pp. 884 - 891
• Main Authors: Murai, Masatoshi, Miyoshi, Hideto
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.07.2016
• Subjects: Binding Sites; Chemical modifications of protein; Complex I; Drug Design; Electron Transport Complex I - antagonists & inhibitors; Electron Transport Complex I - ultrastructure; Enzyme Activation - drug effects; Enzyme Inhibitors - chemistry; Inhibitors; Models, Chemical; Models, Molecular; Protein Binding; Protein Conformation; Structure-Activity Relationship; Chemical modifications of protein; Complex I; Inhibitors
• ISSN: 0005-2728; 0006-3002; 1879-2650
• DOI: 10.1016/j.bbabio.2015.11.009

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. •We herein focused on recent hot topics on complex I inhibitors.•We also focused on the subjects closely connected to these inhibitors.•Our review may provide useful information not only on the structural and functional aspects of complex I, but also on drug design targeting this enzyme.