Small-Molecule Inhibitors of NADPH Oxidase 4
Small-Molecule Inhibitors of NADPH Oxidase 4
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DOI：
10.1021/jm1004368
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发表时间：
2010-09-23
影响因子：
7.3
通讯作者：
Keri, Gyoergy
中科院分区：
文献类型：
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作者：
Borbely, Gabor;Szabadkai, Istvan;Keri, Gyoergy
NOX酶是许多氧化损伤相关疾病的主要贡献者。不幸的是，目前没有特定的NOX抑制剂可用。在这里，我们描述了新型NOX 4抑制剂的发现和开发。在基于细胞的测定中测试化合物文库作为初级筛选、监测H2O2产生。24种化合物以低微摩尔IC50值抑制NOX 4活性，其中3种被选择用于进一步的药物开发。
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.