Small-molecule inhibitors of NADPH oxidase 4

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 Örfi; György Kéri

doi:10.1021/jm1004368

Small-molecule inhibitors of NADPH oxidase 4

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 Örfi, György Kéri

Chemistry (Twin Cities)

Research output: Contribution to journal › Article › peer-review

50 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	6758-6762
Number of pages	5
Journal	Journal of medicinal chemistry
Volume	53
Issue number	18
DOIs	https://doi.org/10.1021/jm1004368
State	Published - Sep 23 2010

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abstract = "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.",

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AU - Borbély, Gábor

AU - Szabadkai, István

AU - Horváth, Zoltán

AU - Markó, Péter

AU - Varga, Zoltán

AU - Breza, Nóra

AU - Baska, Ferenc

AU - Vántus, Tibor

AU - Huszár, Mónika

AU - Geiszt, Miklós

AU - Hunyady, László

AU - Buday, László

AU - Örfi, László

AU - Kéri, György

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Small-molecule inhibitors of NADPH oxidase 4

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