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Showing 1 to 20 of 31 for “"NQO1"”.
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Improving the Efficacy and Expanding the Application of NQO1-Bioactivated Therapeutics
NADPH:quinone oxidoreductase-1 (NQO1)-bioactivated drugs, such as ß-lapachone (ß-lap), are powerful therapeutics for tumor-specific therapy. They react with NQO1, which is highly overexpressed in most solid tumors, to cause a futile redox cycle that results in devastating oxidative DNA damage and …
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Targeting head and neck squamous cell carcinoma through NQO1-mediated cytotoxicity
… potential in a variety of other solid tumors is NQO1-targeted therapy. In this strategy the overexpression of NQO1 can be taken advantage of by the DNQ derivative IB-DNQ which is a futile substrate for NQO1 that generates high levels of cytotoxic ROS selectively inside the cancer cell. Given the …
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Deoxynyboquinones as NQO1-targeted anticancer compounds and deoxynybomycins as potent and selective antibiotics
Made available in DSpace on 2016-03-02T20:57:24Z (GMT). No. of bitstreams: 5 PARKINSON-DISSERTATION-2015.pdf: 21604741 bytes, checksum: 36ce90169c82a68c9b09739d5545d439 (MD5) LICENSE.txt: 4216 bytes, checksum: 30a9874759f4e96d3a10d148120d7757 (MD5) Parkinson Supplemental 1.pdf: 124148 bytes, …
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NQO1-Bioactivatable Drugs at the Interface of Cancer Metabolism and the DNA Damage Response
… enzyme, NAD(P)H:quinone oxidoreductase-1, NQO1, is dramatically overexpressed in many solid tumor types, including pancreatic ductal adenocarcinoma (PDA) and non-small cell lung cancer (NSCLC). The Boothman laboratory has demonstrated that NQO1 bioactivates a unique class of quinones, such …
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NAD(P)H:QUINONE OXIDOREDUCTASE (NQO1)-DIRECTED LAVENDAMYCIN ANTITUMOR AGENTS: STRUCTURE-BASED DESIGN, MOLECULAR MODELING AND STRUCTURE-ACTIVITY STUDIES
NAD(P)H:quinone oxidoreductase 1 (NQO1) is a two-electron reductase that catalyzes an NAD(P)H-dependent activation of many quinone-based antitumor agents. NQO1, expressed at high levels in many human solid tumors, can be used as a target for enzyme-directed bioreductive antitumor drug development. …
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NAD(P)H:QUINONE OXIDOREDUCTASE (NQO1)-DIRECTED LAVENDAMYCIN ANTITUMOR AGENTS: STRUCTURE-BASED DESIGN, MOLECULAR MODELING AND STRUCTURE-ACTIVITY STUDIES
NAD(P)H:quinone oxidoreductase 1 (NQO1) is a two-electron reductase that catalyzes an NAD(P)H-dependent activation of many quinone-based antitumor agents. NQO1, expressed at high levels in many human solid tumors, can be used as a target for enzyme-directed bioreductive antitumor drug development. …
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In-depth bioinformatics analysis of the phosphoproteome of triple negative breast cancer treated with a tumor selective NQO1 bioactivatable drug
… agent IB-DNQ (isobutyl-deoxyniboquinone). NQO1 or NADPH:quinone oxidoreductase-1 is a detoxifying enzyme overexpressed in many solid tumors and low expression in normal cells. IB-DNQ is bio-activated by NQO1 enzyme via a futile redox cycling, producing large amounts of reactive oxygen …
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Mechanisms by which natural polyphenols regulate the expression of cytoprotective genes
… examine their effect on Nrf2 and its target gene Nqo1 in rat liver RL-34 and mouse embryonic fibroblast MEF cells. By Nqo1 enzyme activity assay, Western blotting, and Taqman experiments, our study showed that these two flavonoids increased the enzyme activity, protein expression and mRNA level of …
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The Identification and Targeting of Altered NAD+ Metabolism in Glioblastoma
… one such enzyme, NAD(P)H quinone oxidoreductase (NQO1). Elevated expression of NQO1 made GBM cells uniquely sensitive to the NQO1-bioactivatable compound β-lapachone. β-lapachone induced acute DNA damage and NAD+ depletion. However, GBM cells may evade this depletion through activation of NAD+ …
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Structure and function of glutamate transporters
… (gp120) and NAD(P)H:Quinone Oxidoreductase 1 (NQO1). The study of gp120 involved a statistical analysis of substitutions that occur during early infection of clade A HIV, showing that during early infection substitutions are non-random and co-locate in regions associated with receptor binding. …
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Structure and function of glutamate transporters
… (gp120) and NAD(P)H:Quinone Oxidoreductase 1 (NQO1). The study of gp120 involved a statistical analysis of substitutions that occur during early infection of clade A HIV, showing that during early infection substitutions are non-random and co-locate in regions associated with receptor binding. …
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Broccoli bioactives: impact on enzyme induction, estrogen metabolism and human cancer cell growth
… enzyme NAD(P)H dehydrogenase, quinone 1 (NQO1). The present study demonstrated that combinations of purified SF, quercetin and kaempferol increased NQO1 activity in a synergistic manner in murine hepatoma cells. Broccoli is an active accumulator of selenium, and the concentration of this …
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the impact of Ape/Ref1 on hypoxia regulated genes; potential applications for cancer
… the siRNA increases the HIF target, HMOX1 and NQO1,two genes that play key roles in tumor adaptation to a variety of stresses, including anticancer drugs.Ape inhibition activates the NRF2 regulator of redox stress response, which is known to regulate HMOX1 and NQO1. As all these genes are of …
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The development of deoxynyboquinone as a personalized anticancer compound
… in cancer cells relative to healthy cells. NQO1 is a cytoprotective enzyme which is overexpressed in most solid tumors and which detoxifies quinone-containing substrates. However, a few quinones are rendered more toxic by the action of NQO1. We discovered that deoxynyboquinone (DNQ) is a …
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Assessment of synthetic chalcones as cancer chemopreventive agents
… to induction of antioxidant defence gene like NQO1 by detoxifying and reducing oxidative stress. To investigate whether the chalcones can switch on NRF2-ARE pathway, 31 synthetic chalcones were evaluated for (i) their toxicity using thiazolyl blue tetrazolium bromide (MTT) assay, and (ii) …
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Beta-Lapachone Nanotherapeutics for Lung Cancer Therapy
… by the enzyme NAD(P)H:quinone oxidoreductase-1, NQO1, found overexpressed in NSCLC. While promising, its low water solubility limits its clinical translation. Moreovoer, a clinical formulation of the drug proves highly hemolytic and relatively ineffective. Our objective was to develop β-lapachone …
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The Role of Microbiota in Formation and Bioavailability of Sulforaphane From Glucoraphanin in F344 Rats
… the colon is right next to the cecum, colonic NQO1 induction as well as cecal inflammation indicate that cecal microbiota may play an important role in the hydrolysis to bioactive SF from GRP. However, the major detectable hydrolytic product by single Lactobacillus spp. evaluated in our study …
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Azione antiossidante del sulforafane: analisi in cellule cardiache in coltura ed in un modello animale di esercizio fisico
… (GST) and NAD[P]H:quinone oxidoreductase (NQO1) which can function as protectors against oxidative stress. To protect themselves from oxidative stress, cells are equipped with reducing buffer systems including the GSH and thioredoxin (Trx) reductase. GSH is an important tripeptide thiol …
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Enrichment of tomatoes and broccoli with specific bioactives for the reduction of prostate carcinogenesis
… increased activity of colon quinone reductase (NQO1). Indole glucosinolate-enriched broccoli and selenium-enriched broccoli increased hepatic NQO1 and cytochrome P450 1A activity (P < 0.05). Different tomato diets resulted in altered hepatic accumulation of lycopene, phytofluene, and phytoene. …
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THE ROLE OF NRF2 IN PREVENTING OXIDATIVE/ELECTROPHILIC STRESS-INDUCED LIVER INJURY
… through inducing cytoprotective genes including Nqo1 and Gclc, and prevents accumulation of free fatty acids in liver by suppressing the Srebp1 pathway. Oxidative stress also plays an important role in cadmium-induced liver injury. Nrf2-null mice are susceptible, whereas Nrf2-enhanced mice are …
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