title: Small-molecule inhibitors of NADPH oxidase 4.
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.
authors: Vichem Chemie Research Ltd., Budapest, Hungary. gabor.borbely@kkk.org.hu
authors: Gábor
authors: G
authors: Borbély
authors: István
authors: I
authors: Szabadkai
authors: Zoltán
authors: Z
authors: Horváth
authors: Péter
authors: P
authors: Markó
authors: Zoltán
authors: Z
authors: Varga
authors: Nóra
authors: N
authors: Breza
authors: Ferenc
authors: F
authors: Baska
authors: Tibor
authors: T
authors: Vántus
authors: Mónika
authors: M
authors: Huszár
authors: Miklós
authors: M
authors: Geiszt
authors: László
authors: L
authors: Hunyady
authors: László
authors: L
authors: Buday
authors: László
authors: L
authors: Orfi
authors: György
authors: G
authors: Kéri
mesh_terms: D000636:Aminosalicylic Acids / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006861:Hydrogen Peroxide / Q000378:metabolism; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D008958:Models, Molecular; D000074663:NADPH Oxidase 4; D019255:NADPH Oxidases / Q000037:antagonists & inhibitors*; D010070:Oxalates / Q000737:chemistry / Q000494:pharmacology; D010616:Phenanthrenes / Q000138:chemical synthesis / Q000494:pharmacology; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000636:Aminosalicylic Acids; D005419:Flavonoids; D007211:Indoles; D010070:Oxalates; D010616:Phenanthrenes; D011743:Pyrimidines; D006861:Hydrogen Peroxide; D000074663:NADPH Oxidase 4; D019255:NADPH Oxidases; C498910:NOX4 protein, human