| Small-molecule inhibitors of NADPH oxidase 4. | |
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MedLine Citation:
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PMID: 20731357 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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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Authors:
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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 Orfi; György Kéri |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 53 ISSN: 1520-4804 ISO Abbreviation: J. Med. Chem. Publication Date: 2010 Sep |
Date Detail:
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Created Date: 2010-09-16 Completed Date: 2010-10-11 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: United States |
Other Details:
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Languages: eng Pagination: 6758-62 Citation Subset: IM |
Affiliation:
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Vichem Chemie Research Ltd., Budapest, Hungary. gabor.borbely@kkk.org.hu |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Aminosalicylic Acids
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chemistry,
pharmacology Cell Line Flavonoids / chemistry, pharmacology Humans Hydrogen Peroxide / metabolism Indoles / chemistry, pharmacology Models, Molecular NADPH Oxidase / antagonists & inhibitors* Oxalic Acids / chemistry, pharmacology Phenanthrenes / chemical synthesis, pharmacology Pyrimidines / chemistry, pharmacology Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Aminosalicylic Acids; 0/Flavonoids; 0/Indoles; 0/Oxalic Acids; 0/Phenanthrenes; 0/Pyrimidines; 7722-84-1/Hydrogen Peroxide; EC 1.6.3.-/NOX4 protein, human; EC 1.6.3.1/NADPH Oxidase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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