Literature DB >> 20731357

Small-molecule inhibitors of NADPH oxidase 4.

Gábor Borbély1, 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.   

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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Year:  2010        PMID: 20731357     DOI: 10.1021/jm1004368

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  33 in total

Review 1.  Targeting NOX enzymes in the central nervous system: therapeutic opportunities.

Authors:  Silvia Sorce; Karl-Heinz Krause; Vincent Jaquet
Journal:  Cell Mol Life Sci       Date:  2012-05-30       Impact factor: 9.261

Review 2.  Therapeutic potential of NADPH oxidase 1/4 inhibitors.

Authors:  G Teixeira; C Szyndralewiez; S Molango; S Carnesecchi; F Heitz; P Wiesel; J M Wood
Journal:  Br J Pharmacol       Date:  2016-07-14       Impact factor: 8.739

3.  High-Throughput Screening of NOX Inhibitors.

Authors:  Jacek Zielonka; Monika Zielonka; Gang Cheng; Micael Hardy; Balaraman Kalyanaraman
Journal:  Methods Mol Biol       Date:  2019

4.  Recent Developments in the Probes and Assays for Measurement of the Activity of NADPH Oxidases.

Authors:  Jacek Zielonka; Micael Hardy; Radosław Michalski; Adam Sikora; Monika Zielonka; Gang Cheng; Olivier Ouari; Radosław Podsiadły; Balaraman Kalyanaraman
Journal:  Cell Biochem Biophys       Date:  2017-06-29       Impact factor: 2.194

5.  Design, synthesis, and biological evaluation of inhibitors of the NADPH oxidase, Nox4.

Authors:  Qian Xu; Amol A Kulkarni; Ayyiliath M Sajith; Dilbi Hussein; David Brown; Osman F Güner; M Damoder Reddy; E Blake Watkins; Bernard Lassègue; Kathy K Griendling; J Phillip Bowen
Journal:  Bioorg Med Chem       Date:  2017-12-17       Impact factor: 3.641

Review 6.  Targeting NOX enzymes in pulmonary fibrosis.

Authors:  Louise Hecker; Jeff Cheng; Victor J Thannickal
Journal:  Cell Mol Life Sci       Date:  2012-05-23       Impact factor: 9.261

Review 7.  Evolution of NADPH Oxidase Inhibitors: Selectivity and Mechanisms for Target Engagement.

Authors:  Sebastian Altenhöfer; Kim A Radermacher; Pamela W M Kleikers; Kirstin Wingler; Harald H H W Schmidt
Journal:  Antioxid Redox Signal       Date:  2014-02-26       Impact factor: 8.401

8.  The Nox4 inhibitor GKT137831 attenuates hypoxia-induced pulmonary vascular cell proliferation.

Authors:  David E Green; Tamara C Murphy; Bum-Yong Kang; Jennifer M Kleinhenz; Cédric Szyndralewiez; Patrick Page; Roy L Sutliff; C Michael Hart
Journal:  Am J Respir Cell Mol Biol       Date:  2012-08-16       Impact factor: 6.914

9.  Cytotoxic activities of substituted 3-(3,4,5-trimethoxybenzylidene)-1,3-dihydroindol-2-ones and studies on their mechanisms of action.

Authors:  Aldo Andreani; Massimiliano Granaiola; Alessandra Locatelli; Rita Morigi; Mirella Rambaldi; Lucilla Varoli; Francesco Vieceli Dalla Sega; Cecilia Prata; Tam L Nguyen; Ruoli Bai; Ernest Hamel
Journal:  Eur J Med Chem       Date:  2013-04-03       Impact factor: 6.514

10.  Fulvene-5 inhibition of Nadph oxidases attenuates activation of epithelial sodium channels in A6 distal nephron cells.

Authors:  David Trac; Bingchen Liu; Alan C Pao; Sheela V Thomas; Michael Park; Charles A Downs; He-Ping Ma; My N Helms
Journal:  Am J Physiol Renal Physiol       Date:  2013-07-17
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