Activity-based probes for studying the activity of flavin-dependent oxidases and for the protein target profiling of monoamine oxidase inhibitors

Joanna M Krysiak; Johannes Kreuzer; Peter Macheroux; Albin Hermetter; Stephan A Sieber; Rolf Breinbauer

doi:10.1002/anie.201201955

Activity-based probes for studying the activity of flavin-dependent oxidases and for the protein target profiling of monoamine oxidase inhibitors

Angew Chem Int Ed Engl. 2012 Jul 9;51(28):7035-40. doi: 10.1002/anie.201201955. Epub 2012 Jun 11.

Authors

Joanna M Krysiak¹, Johannes Kreuzer, Peter Macheroux, Albin Hermetter, Stephan A Sieber, Rolf Breinbauer

Affiliation

¹ Institute of Organic Chemistry, Graz University of Technology, Austria.

Abstract

High profile: new activity-based protein profiling (ABPP) probes have been designed that target exclusively monoamine oxidases A and B within living cells (see picture; FAD=flavin adenine dinucleotide, FMN=flavin monodinucleotide). With these probes it could be shown that the MAO inhibitor deprenyl, which is in clinical use against Parkinson's disease, shows unique protein specificity despite its covalent mechanism of action.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Brain Neoplasms / drug therapy*
Brain Neoplasms / enzymology*
Flavin Mononucleotide / metabolism
Flavin-Adenine Dinucleotide / metabolism
Humans
Monoamine Oxidase / chemistry*
Monoamine Oxidase / metabolism
Monoamine Oxidase Inhibitors / pharmacology*
Selegiline / pharmacology*
Tumor Cells, Cultured

Substances

Monoamine Oxidase Inhibitors
Flavin-Adenine Dinucleotide
Selegiline
Flavin Mononucleotide
Monoamine Oxidase