Document Detail


Small-molecule inhibitors of NADPH oxidase 4.
MedLine Citation:
PMID:  20731357     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
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:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  53     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-09-16     Completed Date:  2010-10-11     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  6758-62     Citation Subset:  IM    
Affiliation:
Vichem Chemie Research Ltd., Budapest, Hungary. gabor.borbely@kkk.org.hu
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MeSH Terms
Descriptor/Qualifier:
Aminosalicylic Acids / 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:
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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