2. Academic Validation
  3. Small-molecule inhibitors of NADPH oxidase 4

Small-molecule inhibitors of NADPH oxidase 4

  • J Med Chem. 2010 Sep 23;53(18):6758-62. doi: 10.1021/jm1004368.
Gábor Borbély 1,  István Szabadkai,  Zoltán Horváth,  Péter Markó,  Zoltán Varga,  Nóra Breza,  Ferenc Baska,  Tibor Vántus,  Mónika Huszár,  Miklós Geiszt,  László Hunyady,  László Buday,  László Orfi,  György Kéri
Affiliations

Affiliation

  • 1 Vichem Chemie Research Ltd., Budapest, Hungary. gabor.borbely@kkk.org.hu
PMID: 20731357 DOI: 10.1021/jm1004368
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 IC(50) values of which three were selected for further drug development.

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