重组
expressed in E. coli
质量水平
检测方案
≥90% (SDS-PAGE)
形式
lyophilized powder
比活
≥100 units/mg protein
分子量
monomer 31000
UniProt登记号
储存温度
2-8°C
基因信息
human ... NQO1(1728)
应用
人双硫腙酶已用于研究评估新型醌磷二酰胺前药的开发。人DT黄递酶也被用于研究其晶体结构，以开发其与细胞毒性前体药物5-（氮丙啶-1-基）-2，4-二硝基苯甲酰胺（CB1954）相互作用的模型。
生化/生理作用
NQO1是一种胞质同型二聚体FAD依赖酶，催化大量细胞毒性醌类减少，从而保护细胞免受氧化应激。此外，氧化应激也可能增强NQO1介导的p53和p73对蛋白酶体降解的保护。NQO1的高诱导表达受Nrf2-Keap1/ARE通路控制，似乎受氧化应激敏感性变化的影响。在缺氧无糖期间，NQO1似乎参与了AMPK诱导的癌细胞死亡。 NQO1在多种实体瘤（包括乳腺癌、胰腺癌、肺癌和结肠癌等）中均有过度表达。
双硫腙酶，也称为NAD（P）H：（醌受体）氧化还原酶，参与几种细胞毒性抗肿瘤醌类和硝基苯类的还原活化过程。它使用NADH或NADPH作为电子供体，催化醌类和醌类化合物的双电子还原成氢醌类。黄素酶每摩尔酶含有1摩尔FAD。
显示体内激活醌基抗肿瘤剂。适合与载体分子结合。
单位定义
一个单位将在37℃甲萘醌底物存在下每min/mg还原1.0 & # 956；摩尔细胞色素C
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
法规信息
常规特殊物品
Molecular of Modelling of Human DT-Diaphorase for Enzyme-Directed Bioreductive Drug Design.
Doughtyl, S.W. and Phillips, R.M.
Molecular Simulations, 24, 209-209 (2000)
C Flader et al.
Journal of medicinal chemistry, 43(16), 3157-3167 (2000-08-24)
A series of naphthoquinone and benzimidazolequinone phosphorodiamidates has been synthesized and studied as potential cytotoxic prodrugs activated by DT-diaphorase. Reduction of the quinone moiety in the target compounds was expected to provide a pathway for expulsion of the phosphoramide mustard
David Siegel et al.
Frontiers in pharmacology, 13, 1015642-1015642 (2022-11-22)
The stress induced protein NQO1 can participate in a wide range of biological pathways which are dependent upon the interaction of NQO1 with protein targets. Many of the protein-protein interactions involving NQO1 have been shown to be regulated by the
Yang Yang et al.
Journal of experimental & clinical cancer research : CR, 33, 14-14 (2014-02-07)
NAD (P) H: quinone oxidoreductase 1 (NQO1) is a xenobiotic metabolizing enzyme that detoxifies chemical stressors and antioxidants, providing cytoprotection in normal tissues. However, high-level expression of NQO1 has been correlated with numerous human malignancies, suggesting a role in carcinogenesis
S Chen et al.
The Journal of biological chemistry, 272(3), 1437-1439 (1997-01-17)
DT-diaphorase (EC 1.6.99.2), also referred to as NAD(P)H:(quinone-acceptor) oxidoreductase, is involved in the reductive activation process of several cytotoxic antitumor quinones and nitrobenzenes. It has been observed in our and other laboratories that the rat enzyme is significantly more effective
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