Small-Molecule Inhibitors of NADPH Oxidase 4

被引：47

作者：

Borbely, Gabor ^{[1
,2
]}

Szabadkai, Istvan ^{[1
]}

Horvath, Zoltan ^{[1
]}

Marko, Peter ^{[1
]}

Varga, Zoltan ^{[1
]}

Breza, Nora ^{[1
]}

Baska, Ferenc ^{[1
,2
]}

Vantus, Tibor ^{[4
]}

Huszar, Monika ^{[4
]}

Geiszt, Miklos ^{[5
]}

Hunyady, Laszlo ^{[5
]}

Buday, Laszlo ^{[6
]}

Orfi, Laszlo ^{[1
,2
,3
]}

Keri, Gyoergy ^{[1
,2
,4
]}

机构：

[1] Vichem Chem Res Ltd, Budapest, Hungary

[2] Semmelweis Univ, Rat Drug Design Lab CRC, H-1085 Budapest, Hungary

[3] Semmelweis Univ, Dept Pharmaceut Chem, H-1085 Budapest, Hungary

[4] Semmelweis Univ, Dept Med Chem, Hungarian Acad Sci, Pathobiochem Res Grp, H-1085 Budapest, Hungary

[5] Semmelweis Univ, Fac Med, Dept Physiol, H-1085 Budapest, Hungary

[6] Hungarian Acad Sci, Biol Res Ctr, Inst Enzymol, Budapest, Hungary

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 18期

关键词：

TYROSINE KINASE; PROTEIN-KINASE; APIGENIN;

D O I：

10.1021/jm1004368

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 IC50 values of which three were selected for further drug development.

引用

页码：6758 / 6762

页数：5

共 50 条

[1] Inhibition of lysyl oxidase in breast cancer cells by small-molecule inhibitors
Johnston, Kathryn
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2017, 254
[2] Small-molecule allosteric inhibitors of GPX4
Liu, Hengrui
Forouhar, Farhad
Lin, Annie J.
Wang, Qian
Polychronidou, Vasiliki
Soni, Rajesh Kumar
Xia, Xin
Stockwell, Brent R.
CELL CHEMICAL BIOLOGY, 2022, 29 (12) : 1680 - +
[3] Small-molecule caspase inhibitors
Zhenodarova, S. M.
RUSSIAN CHEMICAL REVIEWS, 2010, 79 (02) : 119 - 143
[4] Small-molecule arginase inhibitors
Ivanenkov, Yan A.
Chufarova, Nina V.
PHARMACEUTICAL PATENT ANALYST, 2014, 3 (01) : 65 - 85
[5] Small-molecule enzyme inhibitors
Edwards, P
DRUG DISCOVERY TODAY, 2001, 6 (03) : 160 - 160
[6] Small-Molecule NOX Inhibitors: ROS-Generating NADPH Oxidases as Therapeutic Targets
Jaquet, Vincent
Scapozza, Leonardo
Clark, Robert A.
Krause, Karl-Heinz
Lambeth, J. David
ANTIOXIDANTS & REDOX SIGNALING, 2009, 11 (10) : 2535 - 2552
[7] Small-Molecule Inhibitors Targeting eIF4A in Leukemia
Jia, Xiaofeng
Zhou, Hong
CURRENT PROTEIN & PEPTIDE SCIENCE, 2021, 22 (07) : 559 - 566
[8] Advances in the Discovery of Small-Molecule IRAK4 Inhibitors
Hynes, John, Jr.
Nair, Satheesh K.
ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 49, 2014, 49 : 117 - 133
[9] Small-molecule inhibitors of carboxylesterase Notum
Zhao, Yuguang
Jolly, Sarah
Benvegnu, Stefano
Jones, E. Yvonne
Fish, Paul, V
FUTURE MEDICINAL CHEMISTRY, 2021, 13 (11) : 1001 - 1015
[10] Probing Translation with Small-Molecule Inhibitors
Blanchard, Scott C.
Cooperman, Barry S.
Wilson, Daniel N.
CHEMISTRY & BIOLOGY, 2010, 17 (06): : 633 - 645

← 1 2 3 4 5 →