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Small-Molecule Inhibitors of NADPH Oxidase 4

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journal contribution
posted on 23.09.2010, 00:00 authored by Gábor Borbély, István Szabadkai, Zoltán Horváth, Péter Markó, Zoltán Varga, Nóra Breza, Ferenc Baska, Tibor Vántus, Mónika Huszár, Miklós Geiszt, László Hunyady, László Buday, László Őrfi, György Kéri
NOX enzymes are the major contributors in many oxidative damage related diseases. Unfortunately, at present no specific NOX inhibitor is available. Here, we describe the discovery and development of novel NOX4 inhibitors. Compound libraries were tested in a cell-based assay as a primary screen, monitoring H2O2 production. Twenty-four compounds inhibited Nox4 activity with low-micromolar IC50 values of which three were selected for further drug development.