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Showing 1-30 of 61 results for "N5757" within Papers
Gui-Zhen Wang et al.
Nature communications, 10(1), 1125-1125 (2019-03-10)
Whether tobacco carcinogens enable exposed cells immune escape resulting in carcinogenesis, and why patients who smoke respond better to immunotherapies than non-smokers, remains poorly understood. Here we report that cigarette smoke and the carcinogen benzo(a)pyrene (BaP) induce PD-L1 expression on
An Wang et al.
The Journal of biological chemistry, 286(7), 5736-5743 (2010-12-15)
The atomic structure of human P450 1B1 was determined by x-ray crystallography to 2.7 Å resolution with α-naphthoflavone (ANF) bound in the active site cavity. Although the amino acid sequences of human P450s 1B1 and 1A2 have diverged significantly, both
Ioana Ferecatu et al.
Particle and fibre toxicology, 7, 18-18 (2010-07-29)
Nowadays, effects of fine particulate matter (PM2.5) are well-documented and related to oxidative stress and pro-inflammatory response. Nevertheless, epidemiological studies show that PM2.5 exposure is correlated with an increase of pulmonary cancers and the remodeling of the airway epithelium involving
Jayme P Coyle et al.
Particle and fibre toxicology, 17(1), 40-40 (2020-08-14)
Engineered nanomaterials are increasingly being incorporated into synthetic materials as fillers and additives. The potential pathological effects of end-of-lifecycle recycling and disposal of virgin and nano-enabled composites have not been adequately addressed, particularly following incineration. The current investigation aims to
Lin He et al.
Bioorganic & medicinal chemistry letters, 20(20), 6008-6012 (2010-09-14)
Our kinetics studies demonstrated that the nature product chrysin exhibited a high inhibitory affinity of 54 nM towards human cytochrome P450 1A2 and was comparable to α-naphthoflavone (49 nM), whereas it represented a moderate affinity of 5225 nM against human
Le P Ngo et al.
Cell reports, 26(6), 1668-1678 (2019-02-07)
Cell survival is a critical and ubiquitous endpoint in biology. The broadly accepted colony formation assay (CFA) directly measures a cell's ability to divide; however, it takes weeks to perform and is incompatible with high-throughput screening (HTS) technologies. Here, we
You-Jung Hwang et al.
Toxicology letters, 225(1), 130-138 (2013-12-03)
Immune system dysfunctions including the increased Th1/Th2 ratio are common in chronic kidney disease (CKD) patients, and a wide variety of skin diseases including Th1-mediated uremic pruritis are associated with CKD. Although there are more than 90 uremic toxins reported
Barbara M Zietek et al.
SLAS discovery : advancing life sciences R & D, 23(3), 283-293 (2017-12-22)
With early assessment of inhibitory properties of drug candidates and their circulating metabolites toward cytochrome P450 enzymes, drug attrition, especially later in the drug development process, can be decreased. Here we describe the development and validation of an at-line nanofractionation
G J Diaz et al.
British poultry science, 51(6), 828-837 (2010-12-17)
1. A study was conducted to determine the cytochrome P450 enzymes responsible for the bioactivation of aflatoxin B1 into its epoxide form (AFBO) in turkey liver microsomes. 2. The strategies used included the measurement of prototype substrate activity for specific
Julia Dinger et al.
Toxicology letters, 241, 82-94 (2015-11-26)
New psychoactive substances (NPS) are not tested for their cytochrome P450 (CYP) inhibition potential before consumption. Therefore, this potential was explored for tryptamine-derived NPS (TDNPS) including alpha-methyl tryptamines (AMTs), dimethyl tryptamines (DMTs), diallyl tryptamines (DALTs), and diisopropyl tryptamines (DiPTs) using
Julia Dinger et al.
Archives of toxicology, 90(2), 305-318 (2014-11-25)
In vitro cytochrome P450 (CYP) inhibition assays are common approaches for testing the inhibition potential of drugs for predicting potential interactions. In contrast to marketed medicaments, drugs of abuse, particularly the so-called novel psychoactive substances, were not tested before distribution
Qiqiang He et al.
International journal of clinical and experimental pathology, 6(2), 168-178 (2013-01-19)
α-Naphthoflavone (α-NF) is a synthetic flavonone derivative and is well known as a potent inhibitor of aromatase in a variety of systems. However, its role in lipid metabolism remains far from understood. The aim of current study was to investigate
Roger J Griffin et al.
Journal of medicinal chemistry, 48(2), 569-585 (2005-01-22)
A diverse range of chromen-2-one, chromen-4-one and pyrimidoisoquinolin-4-one derivatives was synthesized and evaluated for inhibitory activity against the DNA repair enzyme DNA-dependent protein kinase (DNA-PK), with a view to elucidating structure-activity relationships for potency and kinase selectivity. DNA-PK inhibitory activity
Abdullah Mayati et al.
Environmental toxicology, 27(9), 556-562 (2011-04-01)
Polycyclic aromatic hydrocarbons (PAHs) such as benzo(a)pyrene (B(a)P) constitute a major family of widely-distributed environmental toxic contaminants, known as potent ligands of the aryl hydrocarbon receptor (AhR). B(a)P has been recently shown to trigger an early and transient increase of
Carolina B Moraes et al.
SLAS discovery : advancing life sciences R & D, 24(3), 346-361 (2019-02-21)
According to the World Health Organization, more than 1 billion people are at risk of or are affected by neglected tropical diseases. Examples of such diseases include trypanosomiasis, which causes sleeping sickness; leishmaniasis; and Chagas disease, all of which are
Sun Min Lim et al.
Anticancer research, 33(6), 2499-2508 (2013-06-12)
To investigate mechanisms of discrepancy in response to a MEK/ERK inhibitor, U0126, in KRAS- and BRAF-mutant colorectal cancer cells. Multiparametric flow cytometry was performed on two colon cancer cell lines, HCT116 and HT29. Cells were treated with U0126, and phospho-specific
Julia Dinger et al.
Analytical and bioanalytical chemistry, 406(18), 4453-4464 (2014-05-17)
Knowledge about the cytochrome P450 (CYP) inhibition potential of new drug candidates is important for drug development because of its risk of interactions. For novel psychoactive substances (NPS), corresponding data are not available. For developing a general drug inhibition cocktail
Leonard Blum et al.
Scientific reports, 10(1), 7534-7534 (2020-05-07)
Parasite-mediated diseases like malaria and schistosomiasis are growing health problems worldwide and novel drug candidates are urgently needed. In this study, the in-vitro safety profile of steroid compound 1o (sc1o), effective against the parasites Plasmodium falciparum and Schistosoma mansoni with
Anne Van Vlaslaer et al.
EJNMMI research, 3(1), 10-10 (2013-02-15)
11C-PiB has been developed as a positron-emission tomography (PET) ligand for evaluating fibrillar β-amyloid (Aβ) in the human brain. The ligand is rapidly metabolized, with approximately 10% of intact tracer remaining 30 min after injection. When 11C-PiB is used as
Chi-Hao Tsai et al.
Biochimica et biophysica acta. Molecular cell research, 1867(2), 118564-118564 (2019-11-02)
Recently, histone deacetylase inhibitors (HDACi) have become widely used in anti-cancer treatment; however, due to acquired drug resistance and their relatively low specificity, they are largely ineffective against late-stage cancer. Thus, it is critical to elucidate the molecular mechanisms underlying
Bikash Dangi et al.
Archives of biochemistry and biophysics, 698, 108677-108677 (2020-11-17)
We investigate the effect of the alcohol-induced increase in the content of CYP2E1 in human liver microsomes (HLM) on the function of CYP3A4. Membrane incorporation of the purified CYP2E1 into HLM considerably increases the rate of metabolism of 7-benzyloxyquinoline (BQ)
Yong-Xian Shao et al.
European biophysics journal : EBJ, 41(3), 297-306 (2012-01-10)
In our previous kinetics studies the natural products oroxylin and wogonin were shown to have strong biological affinity for, and inhibitory effects against, human cytochrome P450 1A2, with IC(50) values of 579 and 248 nM, respectively; this might lead to
Ying-Yuan Lu et al.
Xenobiotica; the fate of foreign compounds in biological systems, 47(8), 667-672 (2016-12-03)
1. The aim of this study was to identify the hepatic metabolic enzymes, which involved in the biotransformation of 6-benzyl-1-benzyloxymethyl-5-iodouracil (W-1), a novel non-nucleoside reverse transcriptase inhibitor (NNRTI) in rat and human in vitro. 2. The parent drug of W-1 was incubated
Man Zhang et al.
Journal of ethnopharmacology, 251, 112549-112549 (2020-01-10)
Inflammatory bowel disease (IBD) is one of the most common chronic inflammatory illnesses of the gastrointestinal tract due to the imbalance of immune homeostasis of T helper cells and/or regulatory T cells (Tregs). The Traditional Chinese medicine herb has been
Cintia Scucuglia Heluany et al.
Toxicology, 408, 22-30 (2018-06-25)
Robust correlation between the severity of rheumatoid arthritis (RA) and cigarette smoking has been clinically demonstrated. Nevertheless, cigarette compounds responsible for this toxic effect and their mechanisms have not been described. Considering that hydroquinone (HQ) is an abundant, pro-oxidative compound
Xiaoxi Yang et al.
Toxicology letters, 312, 139-147 (2019-05-15)
As the most toxic dioxin, 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) has gained lots of concerns, due to its diverse deleterious effects. However, the knowledge on carcinogenic risk of TCDD during early stage of development remains scarce. The in vivo teratoma formation model based
M D Chanyshev et al.
Biomeditsinskaia khimiia, 58(3), 310-317 (2012-08-04)
We have investigated the effect of polycyclic aromatic hydrocarbons (PAHs) on estrogen-metabolizing genes CYP1A1, CYP1B1, CYP19 and ERalpha and cyclin D1 genes, which control of cell division in estrogen-depended tissues. Treatment of rats with benzo(a)pyren (BP) or 3-methylcholantrene (MC) significantly
Makoto Matsumoto et al.
PLoS medicine, 3(11), e466-e466 (2006-11-30)
Tuberculosis (TB) is still a leading cause of death worldwide. Almost a third of the world's population is infected with TB bacilli, and each year approximately 8 million people develop active TB and 2 million die as a result. Today's
Daniel J Frank et al.
The Journal of biological chemistry, 286(7), 5540-5545 (2010-12-24)
Cytochrome P450 3A4 (CYP3A4) displays non-Michaelis-Menten kinetics for many of the substrates it metabolizes, including testosterone (TST) and α-naphthoflavone (ANF). Heterotropic effects between these two substrates can further complicate the metabolic profile of the enzyme. In this work, monomeric CYP3A4
Flavia Girolami et al.
Toxicology letters, 206(2), 204-209 (2011-08-02)
The exposure to dioxin-like (DL) compounds, an important class of persistent environmental pollutants, results in the altered expression of target genes. This occurs through the binding to the aryl hydrocarbon receptor (AhR), the subsequent dimerization with the AhR nuclear translocator
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