N5757

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Development and validation of a liquid-chromatography high-resolution tandem mass spectrometry approach for quantification of nine cytochrome P450 (CYP) model substrate metabolites in an in vitro CYP inhibition cocktail.

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

Aza-PBHA, a potent histone deacetylase inhibitor, inhibits human gastric-cancer cell migration via PKCα-mediated AHR-HDAC interactions.

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

In-vitro safety and off-target profile of the anti-parasitic arylmethylaminosteroid 1o.

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

Combination of CYP inhibitor with MEK/ERK inhibitor enhances the inhibitory effect on ERK in BRAF mutant colon cancer cells.

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

Profiling of hepatic clearance pathways of Pittsburgh compound B and human liver cytochrome p450 phenotyping.

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

Aryl hydrocarbon receptor-independent up-regulation of intracellular calcium concentration by environmental polycyclic aromatic hydrocarbons in human endothelial HMEC-1 cells.

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

Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform.

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

Cytochrome P450 inhibition potential of new psychoactive substances of the tryptamine class.

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

Nanofractionation Platform with Parallel Mass Spectrometry for Identification of CYP1A2 Inhibitors in Metabolic Mixtures.

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

Bioactivation of aflatoxin B1 by turkey liver microsomes: responsible cytochrome P450 enzymes.

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

Uremic toxin indoxyl 3-sulfate regulates the differentiation of Th2 but not of Th1 cells to lessen allergic asthma.

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

Isoform-selective inhibition of chrysin towards human cytochrome P450 1A2. Kinetics analysis, molecular docking, and molecular dynamics simulations.

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

Microcolony Size Distribution Assay Enables High-Throughput Cell Survival Quantitation.

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

Effects of alcohol-induced increase in CYP2E1 content in human liver microsomes on the activity and cooperativity of CYP3A4.

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)

The molecular basis for the inhibition of human cytochrome P450 1A2 by oroxylin and wogonin.

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

Polycyclic aromatic hydrocarbon components contribute to the mitochondria-antiapoptotic effect of fine particulate matter on human bronchial epithelial cells via the aryl hydrocarbon receptor.

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

Carbon nanotube filler enhances incinerated thermoplastics-induced cytotoxicity and metabolic disruption in vitro.

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

Structural characterization of the complex between alpha-naphthoflavone and human cytochrome P450 1B1.

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

The Aryl hydrocarbon receptor mediates tobacco-induced PD-L1 expression and is associated with response to immunotherapy.

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

In vitro cytochrome P450 inhibition potential of methylenedioxy-derived designer drugs studied with a two-cocktail approach.

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

Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.

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

α-Naphthoflavone inhibits 3T3-L1 pre-adipocytes differentiation via modulating p38MAPK signaling.

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

CYP enzymes, expressed within live human suspension cells, are superior to widely-used microsomal enzymes in identifying potent CYP1A1/CYP1B1 inhibitors: Identification of quinazolinones as CYP1A1/CYP1B1 inhibitors that efficiently reverse B[a]P toxicity and cisplatin resistance.

Vinay R Sonawane et al.

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 131, 177-194 (2019-02-19)

Microsomal cytochrome P450 (CYP) enzymes, isolated from recombinant bacterial/insect/yeast cells, are extensively used for drug metabolism studies. However, they may not always portray how a developmental drug would behave in human cells with intact intracellular transport mechanisms. This study emphasizes

Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).

Yagmur Muftuoglu et al.

Bioorganic & medicinal chemistry letters, 20(10), 3050-3064 (2010-04-24)

The present study utilizes for the first time the structural information of aromatase, an important pharmacological target in anti-breast cancer therapy, to extract the pharmacophoric features important for interactions between the enzyme and its substrate, androstenedione. A ligand-based pharmacophore model

Effect of diammonium glycyrrhizinate on pharmacokinetics of omeprazole by regulating cytochrome P450 enzymes and plasma protein binding rate.

Lu Han et al.

Xenobiotica; the fate of foreign compounds in biological systems, 49(8), 975-980 (2018-09-15)

1. In clinical practice, diammonium glycyrrhizinate is usually used with omeprazole in patients with viral hepatitis and cirrhosis accompanied by peptic ulcers. However, the drug interaction between diammonium glycyrrhizinate and omeprazole remains unclear. 2. In this study, the effects of

Potential cancer chemopreventive in vitro activities of monomeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis.

Anja Krick et al.

Journal of natural products, 70(3), 353-360 (2007-02-13)

Investigation of the fungal strain Monodictys putredinis isolated from the inner tissue of a marine green alga led to the isolation of four new monomeric xanthones and a benzophenone. All structures were elucidated by extensive spectroscopic measurements. The relative configuration

Aryl hydrocarbon receptor activation and CYP1A induction by cooked food-derived carcinogenic heterocyclic amines in human HepG2 cell lines.

Masashi Sekimoto et al.

Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 97, 256-264 (2016-10-30)

The ability of nine cooked food-derived heterocyclic aromatic amines (HCAs), such as 3-amino-1,4-dimethyl-5H-pyrido[4,3-b]indole (Trp-P-1), 3-amino-1-methyl-5H-pyrido[4,3-b]indole (Trp-P-2), 2-amino-6-methylpyrido[12-a:3',2'-d]imidazole (Glu-P-1), 2-amino-pyrido[12-a:3',2'-d]imidazole hydrochloride (Glu-P-2), 2-amino-9H-pyrido[2,3-b]indole (AαC), 2-amino-3-methyl-9H-pyrido[2,3-b]indole (MeAαC), 2-amino-3-methylimidazo[4,5-f]quinolone (IQ), 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx) and 2-amino-1-methyl-6-phenyl-1H-imidazo[4,5-b]pyridine (PhIP), to activate human aryl hydrocarbon receptor (hAhR) was

Hepatic cytochrome P450s attenuate the cytotoxicity induced by leflunomide and its active metabolite A77 1726 in primary cultured rat hepatocytes.

Qiang Shi et al.

Toxicological sciences : an official journal of the Society of Toxicology, 122(2), 579-586 (2011-05-07)

The Black Box Warning section of the U.S. drug label for leflunomide was recently updated to include stronger warnings about potential hepatotoxicity from this novel anti-arthritis drug. Because metabolic activation is a key mechanism for drug-induced hepatotoxicity, we examined whether

Effects of cytochrome P450 inhibitors on peroxidase activity.

Marketa Martinkova et al.

Neuro endocrinology letters, 33 Suppl 3, 33-40 (2013-01-29)

Of several enzymes metabolizing xenobiotics, cytochrome P450 (CYP) and peroxidase enzymes seem to be most important. One of the major challenges in studies investigating metabolism of xenobiotics is to resolve which of these two groups of enzymes is predominant to

Metabolism and Bioactivation of Corynoline With Characterization of the Glutathione/Cysteine Conjugate and Evaluation of Its Hepatotoxicity in Mice.

Ruijuan Liu et al.

Frontiers in pharmacology, 9, 1264-1264 (2018-11-22)

Corynoline (CRL), an isoquinoline alkaloid, is the major constituent derived from Corydalis bungeana Herba, which is a well-known Chinese herbal medicine widely used in many prescriptions. The purpose of this study was to comprehensively investigate the metabolism and bioactivation of

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