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biotechnology
the flavoprotein WrbA from Escherichia coli represents a new family of multimeric flavodoxin-like proteins implicated in cell protection against oxidative stress, WrbA has NAD(P)H: quinone reductase activity, forms multimers and binds FMN only weakly
degradation
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TcpB is acting as a quinone reductase for 6-chlorohydroxyquinone reduction during 2,4,6-trichlorophenol degradation, a toxic pollutant
pharmacology
a series of lavendamycin analogues are tested in docking studies employing an X-ray derived NQO1 active site computational model, structure-based analogue design criteria are valid, resulting in the design of two analogues with high substrate specificity and selective toxicity toward NQO1-rich cells
analysis
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method to measure enzyme inhibition in intact cells based on the resorufin reductase activity of enzyme. Values for 50% inhibition of enzyme by several reported in vivo inhibitors is at least three orders of magnitude higher for intact cells than for cell lysates
analysis
the enzyme is a catalyst for 1,4-dihydronicotinamide adenine dinucleotide-dependent amperometric biosensors and biofuel cells. For NADH detection, a linear range between 0.005 mM and 1 mM, a limit of detection of 0.003 mM, and a high sensitivity can be reached
analysis
development of a functional affinity-based small-molecule probe composed of a potent small-molecule NQO1 inhibitor 4-hydroxy-3-[(2E)-3-(4-hydroxyphenyl)prop-2-enoyl]-2H-1-benzopyran-2-one as the recognition group, a linker and the fluorophores group FITC. The probe exhibits good inhibitory activity of NQO1 and can be used to label the protein in A549 cells at the micromolar level
drug development
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ability of ketoconazole and itraconazole to induce NQO1 gene expression at the transcriptional level through an aryl hydrocarbon receptor-dependent mechanism
drug development
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cytoprotective effect of bromocriptine involving PI3K- and Nrf2-mediated upregulation of the antioxidant enzyme NQO1, which may be a therapeutic strategy to protect cells from oxidative damage in Parkinsons disease
drug development
design of novel lavendamycin analogues with enhanced, selective, and potent antitumor activity
drug development
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greater induction activities of the phase II enzyme quinone reductase associated with stilbenoids serve as a useful starting point for the design of improved chemopreventive agents
drug development
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in vitro, almond skin polyphenols act as antioxidants and induce quinone reductase activity, but these actions are dependent upon their dose, method of extraction, and interaction with antioxidant vitamins
drug development
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induction of phase 2 enzymes, e.g. NQO1 increases resistance to chemical carcinogenesis. Isothiocyanates can therefore be valuable chemopreventative agents, and the specificity of these substances toward the urinary bladder suggest that they may be particularly useful for protecting against bladder cancer
drug development
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mild temperature heat shock elevates the NQO1 expression in cancer cells, which in turn markedly increases the sensitivity of the cells to the bioreductive drug beta-lapachone in vitro and in vivo
drug development
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mild temperature heat shock elevates the NQO1 expression in cancer cells, which in turn markedly increases the sensitivity of the cells to the bioreductive drug beta-lapachone in vitro and in vivo
drug development
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NAD(P)H:quinone oxidoreductase is a major detoxifying enzyme for 7,12-dimethylbenz[a]anthracene. Eugenol has a potent protective effect against 7,12-dimethylbenz[a]anthracene-induced genotoxicity, presumably through the suppression of the 7,12-dimethylbenz[a]anthracene activation and the induction of its detoxification through NAD(P)H:quinone oxidoreductase
drug development
new coumarin-based competitive inhibitors of NQO1. NQO1 inhibition as an anticancer drug design target and superoxide generation as the dicoumarol-mediated mechanism of cytotoxicity
drug development
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the enzyme is a valuable target for activating stimuli-responsive drug delivery systems based on quinone derivatives, such as prodrugs and liposomes
drug development
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mild temperature heat shock elevates the NQO1 expression in cancer cells, which in turn markedly increases the sensitivity of the cells to the bioreductive drug beta-lapachone in vitro and in vivo
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medicine
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activation of antitumor prodrugs
medicine
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acetaminophen is bioactivated by cytochrome P450 to the reactive intermediate N-acetyl-p-benzoquinone imine. Enhanced levels of hepatic enzyme may detoxify N-acetyl-p-benzoquinone imine by reducing it back to acetaminophen
medicine
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antitumour quinones 2,5-diaziridinyl-3-hydroxymethyl-6-methyl-1,4-benzoquinone and 2,5-dimethyl-3,6-diaziridinyl-1,4-benzoquinone, i.e. RH1 and MeDZQ resp., induce apoptosis via enzyme-linked formation of alkylating species rather than via enzyme-linked redox cycling
medicine
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ascorbic acid may potentiate the therapeutic efficacy of As3+ in treatment of acute promyelotic leukemia by enhancing the expression of enzyme together with heme oxygenase-1 and glutathione S-transferase Ya
medicine
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clofibrate-mediated hepatoprotection against acetaminophen does not appear to be dependent upon enhanced expression of enzyme. Conditions of 94% inhobition of enzyme do not increase the susceptibility of hepatocytes from clofibrate treated mice to acetaminophen
medicine
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enzyme is highly upregulated in active and chronic multiple sclerosis lesions, particularly in hypertrophic astrocytes and myelin-laden macrophages
medicine
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enzyme protein is low in normal liver. Livers from patients with damage due to acetaminophen overdose or primary biliary cirrhosis show a strong induction of enzyme protein and activity
medicine
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higher levels of enzyme expression in pancreatic adenocarcinomas compared to nontumourous tissues from nonsmokers. High levels are also found in pancreas of smokers and in pancreatitis tissues. No differences are found in genotype distribution and frequencies of the variant alleles between normal and cancer tissues. Use of enzyme expression as a biomarker for pancreatic cancer
medicine
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presence of significant interethnic differences in polymorphic hepatic enzyme activity. Black donors show about twofold higher enzyme activity than white donors, and cytosolic enzyme activities differ significantly by enzyme genotype status in white, but not in black donors
medicine
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statistically significant risk for colorectal cancer is associated with variant enzyme genotypes
medicine
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NQO1 guards against oxidative stress and carcinogenesis and stabilizes p53, a homozygous common missense variant, NQO1*2, P187S that disables NQO1 predicts poor survival of women with breast cancer, NQO1 deficiency implicates cancer progression and treatment resistance to epirubicin, the NQO1 status is important for the response to epirubicin, ionizing radiation or 5-FU is not, NQO1 genotype is a prognostic and predictive marker for breast cancer
medicine
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NQO1 polymorphism analysis is performed to investigate the relationship between prostate cancer and NQO1 C609T polymorphism in a turkish population, no correlation is found
medicine
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NQO1 polymorphism analysis is performed using genomic DNA from blood samples, NQO1 polymorphisms, C/T and T/T genotypes, are associated with the risk of urothelial cancer, particularly among those who have ever smoked
medicine
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NQO1 polymorphism analysis is performed using genomic DNA from buccal cell samples, anthracycline-related congestive heart failure is an important long-term complication among childhood cancer survivors, NQO1 polymorphism analysis indicated no association between the NQO1 polymorphism and the risk of anthracycline-related congestive heart failure
medicine
NQO1 polymorphism analysis is performed using genomic DNA from rectal biopsy samples, genotypes of C609T, T609T and C609C, G718G, A718A and A718G polymorphisms of NQO1 are compared, C609C genotype shows higher activity, C609T polymorphism is a important predictor for rectal NQO1 activity, fruit and vegetable consumption have no influence on NQO1 activity
medicine
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series of indolequinones are synthesized and tested as inhibitors for NQO1 in pancreatic tumor cells, NQO1 inhibition does not correlate with growth inhibitory activity in MiaPaCa-2 cells
medicine
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3-nitrobenzanthrone is capable to induce NQO1 and CYP1A1 in lungs and kidney of rats thereby enhancing its own genotoxic and carcinogenic potential
medicine
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3H-1,2-dithiole-3-thione potently induces neuronal cellular GSH and NQO1 as well as mitochondrial GSH. Such upregulated endogenous defenses are accompanied by increased resistance to oxidative and electrophilic neurocytotoxicity, e.g. in Parkinson's disease
medicine
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acute manganese intoxication, similarly to that of cadmium and other heavy metals, increases both the hepatic level of Nrf2 and its transfer from the cytoplasm to the nucleus where it actively regulates the induction of phase II enzymes, e.g. NQO1
medicine
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dependence of copper neurotoxicity on DT-diaphorase inhibition
medicine
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exposed workers to benzene in the petroleum refining industry with the T/T genotype for NQO1 show significant 1.9fold and 2.6fold increases in micronuclei and chromosome aberrations frequencies, respectively, compared to controls with C/C and C/T genotypes, after adjusting for age, smoking status, and alcohol intake
medicine
genetic variation, especially the NQO1 609CT polymorphism, is a more important predictor of rectal NQO1 phenotype than fruit and vegetable consumption. White blood cell NQO1 activity is not a good surrogate for rectal activity
medicine
individuals with the NQO1*2 allele are more susceptible to the toxic effects of benzene metabolites. Quinones that are good substrates for human NQO1 are more toxic to the NQO1 containing or expressing tumour cell lines than the NQO1-deficient cell lines. Quinones such as the biphenyl and naphthyl derivatives that are poor substrates show no selectivity or have no measurable cytotoxicity
medicine
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main function of QR1 is probably the detoxification of dietary quinones but it may also contribute to the reduction of vitamin K for its involvement in blood coagluation
medicine
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main function of QR1 is probably the detoxification of dietary quinones but it may also contribute to the reduction of vitamin K for its involvement in blood coagluation
medicine
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main function of QR1 is probably the detoxification of dietary quinones but it may also contribute to the reduction of vitamin K for its involvement in blood coagluation
medicine
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neuroprotective role of DT-diaphorase against aminochrome neurotoxicity
medicine
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no association between NQO1 polymorphism and the risk of anthracycline-related congestive heart failure among childhood cancer survivors
medicine
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NQO1 and SULT1A1 polymorphisms are associated with the risk of urothelial cancer, particularly among those who have ever smoked
medicine
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NQO1 gene polymorphism influences interleukin-6 levels and therefore attenuates the inflammatory response after cardiopulmonary bypass
medicine
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NQO1-induced bioreduction of beta-lap is an essential step in beta-lap-induced cell death. Combined radiotherapy and beta-lap treatment can have a significant effect on human tumor xenografts
medicine
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plays a protective role against the induction of renal tumors by diethylstilbestrol
medicine
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strain difference where Sprague Dawley rats possess a sex-dependent expression and activity of Nqo1 and August Copenhagen x Irish rats exhibit no sexual dimorphism may provide an important tool when using these rat models for oxidative stress and cancer studies
medicine
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synthesis of novel heterocyclic quinones (benzimidazole- and benzothiazole-quinones) as excellent substrates for recombinant human NQO1
medicine
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there is no significant relationship between NQO1 gene C609kT polymorphism and prostate cancer in a Turkish population, but an increased frequency of the TT genotype in patients compared to controls. Carrying the T allele may have an effect on serum prostate specific antigen and alkaline phosphatase levels in prostate cancer patients
medicine
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trend toward lower drug response in patients with the NQO1 null genotype. Inhibiting NQO1 activity decreases p53 levels and drug induced apoptosis in chronic lymphocytic leukemia cells. NQO1 polymorphism may be a risk factor for chronic lymphocytic leukemia especially in males, and a predictor of response to chemotherapy
medicine
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combination therapy employing a member of the group of non-cytotoxic NQO1 inhibitors together with a 2,6-dichlorophenolindophenol-like molecule may provide therapeutic efficacy against tumors that display high NQO1 enzymatic activity
medicine
isoform NQO1-KO mice exhibit a marked increase of permeability and spontaneous inflammation in the gut. In the dextran sulfate sodium salt-induced colitis model, NQO1-KO mice show more severe inflammatory responses than NQO1-wild-type mice. The transcript levels of claudin and occludin, the major tight junction molecules of gut epithelial cells, are significantly decreased in NQO1-KO mice. The colons of NQO1-KO mice also show high levels of reactive oxygen species and histone deacetylase activity
medicine
protein expression but not activity of NQO1 is weakly negatively correlated with age. No sex differences are observed for either protein expression or activity and for ethnicity. Caucasians have greater NQO1 activity than Asians. Overweight children have statistically significantly higher NQO1 activity as compared with ideal weight children
medicine
(+-)-dunnione and its ortho-quinone analogues act as substrates. The biological activity is favored by the presence of methyl group at the C ring and methoxy group at the A ring. The ortho-quinones exert their antitumor activity through NQO1-mediated reactive oxygen species production by redox cycling
medicine
development of an NQO1-targeted radiolabeled agent to establish an internal radiation therapy that amplifies the therapeutic effects when combined with external radiation therapy. The uptake of [125I]-marked compound 3-([[4-iodophenyl]thio]methyl)-5-methoxy-1,2-dimethyl-1H-indole-4,7-dione is specific and is dependent on the expression of NQO1. In NQO1-expressing tumor cells, over 85% of the initial radioactivity of [125I]-marked 3-([[4-iodophenyl]thio]methyl)-5-methoxy-1,2-dimethyl-1H-indole-4,7-dione is observed as an intact form at 1 h after incubation
medicine
in sub-chronic studies upon oral exposure to sulphoraphane for 30 days a 2- to 3fold increase in GSTM1, Gclc and NQO1 transcript levels, and a 2fold increase in NQO1 activity in adult livers is observed
medicine
levels of NQO1 protein and mRNA are significantly elevated in fresh tissue samples of small cell lung cancer. The rate of strong positive NQO1 protein expression is significantly higher in small cell lung cancer when compared with the rate in either adjacent non-cancerous or normal lung tissues and correlated with large tumor size, late pathologic stage and the presence of lymph node metastasis. High?level expression of NQO1 protein is significantly correlated with lower disease-free survival and 5-year survival rates in patients
medicine
low hepatic expression of the active glutathione S-transferases and NQO1 may increase the susceptibility of patients to amodiaquine idiosyncratic hepatotoxicity. NQO1 inactivates protein reactive quinonimines such as amodiaquine by reduction
medicine
natural polymorphism C609T may affect amrubicin-related pharmacokinetics and clinical outcomes in lung cancer treatment. At a dose of 40 mg/m2, the T/T genotype exhibits a tendency toward a relationship with decreased concentrations of amrubicinol on days 2 and 4 of treatment. The genotype also shows a significant decrease of hematological toxicities
medicine
NQO1 is highly expressed in normal melanocytes and in several melanoma cell lines in the presence of wild-type KEAP1, whose mutation elicits constitutive NRF2 activation and resistance to cisplatin. NQO1 expression is dependent on NRF2 activation. Synergistic cytotoxicity of HSP90 inhibitor 17-AAG, i.e. 17-(allylamino)-17-demethoxygeldanamycin, and cisplatin is detected in four out of five NQO1-low cell lines, but not in a cell line with KEAP1 mutation
medicine
NQO1 overexpression induces hepatocellular carcinoma cell apoptosis and proliferation inhibition through the AMPK/PGC-1a pathway
medicine
NQO1 overexpression is a main determinant for a potential chemotherapy resistance or an increased sensitivity to quinone-bearing compounds
medicine
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clofibrate-mediated hepatoprotection against acetaminophen does not appear to be dependent upon enhanced expression of enzyme. Conditions of 94% inhobition of enzyme do not increase the susceptibility of hepatocytes from clofibrate treated mice to acetaminophen
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additional information
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ERbeta and hPMC2 are required for trans-hydroxytamoxifen-dependent recruitment of coactivators such as PARP-1 to the electrophile response element of NQO1 resulting in the induction of the antioxidative enzyme and subsequent protection against oxidative DNA damage
additional information
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oxidative stress-type cytotoxicity of chromate in FLK cells may be partly attributed to its reduction by NQO1, but not by glutathione reductase
additional information
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PIFI is a novel component essential for NDH-mediated nonphotochemical reduction of the plastoquinone pool in chlororespiratory electron transport
additional information
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WrbA bridges flavodoxins and oxidoreductases. WrbA shows a close relationship to mammalian Nqo1