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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
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)
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Hidesuke Fukazawa et al.
Biological & pharmaceutical bulletin, 35(8), 1320-1327 (2012-08-07)
We describe a cell-based, microplate colorimetric screen for anti-hepatitis C virus (HCV) drugs that exploits the HCV-JFH1 viral culture system. Antiviral activity was assessed by measuring protection against the HCV-JFH1-induced cytopathic effect (CPE) in Huh7.5.1 cells using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide
Miroslav Dostalek et al.
Biomedical papers of the Medical Faculty of the University Palacky, Olomouc, Czechoslovakia, 155(3), 253-257 (2012-01-31)
We previously reported the effect of St John's wort (Hypericum perforatum) standardised extract LI 160 on the activities of cytochrome P450 2C6, 2D2 and 3As (Dostalek et al., Life Sciences 2005;78(3):239-44). In this study, we aimed to assess the effect
Susanne Gauggel-Lewandowski et al.
Chemico-biological interactions, 206(2), 411-422 (2013-06-26)
Due to increasing energy demand and limited fossil fuels, renewable energy sources have gained in importance. Particulate matter (PM) in general, but also PM from the combustion of wood is known to exert adverse health effects in human. These are
Karina A Barreiro et al.
Toxicology and applied pharmacology, 252(1), 11-17 (2011-01-26)
The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor and the first protein involved in a variety of physiological and toxicological processes, including those of xenobiotic metabolizing enzymes. AhR has been found in the ovary of many species and
Soon Young Shin et al.
Bioorganic & medicinal chemistry letters, 21(20), 6036-6041 (2011-09-13)
It has been previously shown that some flavonoids inhibit NF-κB; however, the structure-activity relationships between chalcone, flavanone, flavone, and isoflavone derivatives and their TNFα induced NF-κB inhibitory effects on HCT116 human colon cancer cells have not yet been reported. Therefore
Takeyuki Takamura et al.
Immunology and cell biology, 89(7), 817-822 (2011-02-16)
Increasing evidence suggests that the aryl hydrocarbon receptor (AhR) pathway has an important role in the regulation of inflammatory responses. Most recently, we have shown that the activation of the AhR pathway by a potent AhR agonist inhibits the development
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
Dehui Xu et al.
Biochemical and biophysical research communications, 428(4), 518-524 (2012-11-01)
One of the greatest challenges in multiple myeloma (MM) treatment is to overcome drug resistance. Many pathways are involved including Notch signaling. Notch receptors are expressed by MM cells and Notch ligand Dll1 is present on bone marrow (BM) stromal
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