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Showing 1 to 20 of 21 for “"Cyp1a2"”.
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Stabile Expression von Sulfotransferasen - allein oder in Kombination mit Cytochrom P450 - in Zelllinien für Mutagenitätsuntersuchungen
… die oft durch Cytochrom P450 1A2 (CYP1A2) katalysiert wird. Daran schließt sich eine O-Konjugation durch Sulfotransferasen (SULT) oder N-Acetyltransferasen (NAT) an. Die Bioaktivierung ist ein kritischer Parameter für die Übertragbarkeit von Ergebnissen aus Tiermodellen auf den …
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In vitro metabolism studies to inform physiologically-based pharmacokinetic modelling of mefloquine, ritonavir and proguanil
… the drug was metabolized mainly by CYP3A and CYP1A2. While mefloquine metabolism by CYP3A is widely reported, this is the first report of its metabolism by CYP1A2. Proguanil was found to be metabolized by a number of enzymes, namely CYP1A2, CYP2D6, CYP2C19 and CYP3A. This confirms reported …
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Characterisation of mammalian cytochrome P450 enzymes by their metabolic activities.
… preparations. This suggests the involvement of CYP1A2 in the metabolism of harmine by human liver microsomes. Inhibition studies with selected anti-P450 antibodies and CYP-isoform selective inhibitors indicated extensive inhibition of harmine metabolism by anti-CYPlA antibodies and the CYP1A2 …
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Genetic polymorphisms in breast cancer in relation to risk and prognosis
… post-operative samples from the same patients. CYP1A2*1F C were correlated with a lower ratio at both the pre-and the post-operative visit. Since a high 2-OHE/16αOHE1 ratio has been associated with improved survival the identified factors may modify breast cancer prognosis. In Study III the …
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In search of human cytochrome P450 1A1 enzyme inhibitor
… consists of three members; they are CYP1A1, CYP1A2 and CYP1B1. The mRNAs of CYP1A1 and CYP1B1 genes are known to be expressed in extra-hepatic tissues while that of the CYP1A2 gene is found in the liver amongst other tissues. Under normal circumstances, rarely has CYP1A1 protein expression …
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Studies on pro-oxidant cytochrome P450 enzymes as drug discovery tools and the discovery that they also have a dual function as antioxidants
… the following objectives in mind. (i) CYP1A1, CYP1A2, and CYP1B1 are enzymes highly up-regulated in lung cancers that are caused by inhaling or coming into contact with polyaromatic hydrocarbons (PAHs) which exist in cigarette smoke, in the close proximity to petrochemical industries and in …
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Pharmacogenetics of Efavirenz response in Bantu-speaking South African HIV/AIDS patients
… patients, and is principally metabolised by CYP1A2, CYP2A6, CYP2B6, CYP3A4/5 and the drug transporter ABCB1. Genetic variability in the above genes may contribute to differences in EFV plasma concentrations which affect the levels of viral suppression as well as development of side effects in …
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Genetic polymorphisms in the drug metabolizing genes and their roles in the development of oesophageal cancer
… genes coding for the cytochrome P450 (CYP1A1, CYP1A2, CYP1B1, CYP2E1), sulphotransferase 1A1 (SULT1A1), glutathione S-transferases (GSTT1. GSTM1 and GSTP1) alcohol dehydrogenase (ADH2 and ADH3) and aldehyde dehydrogenase (ALDH2) because the products of these genes are involved in the metabolism …
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The interactions of Propafenone and its enantiomers with the major human forms of cytochrome P450 in terms of inhibition and metabolic rates
… with the major cytochrome P450 isoforms (CYP2D6, CYP1A2, CYP3A4 and CYP2C19) to determine any stereospecific differences which may exist. This was conducted by measuring the in vitro metabolism of propafenone (racemate and enatiomers) and by developing CYP inhibition screens which could prove to …
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Xenobiotic Metabolism Genes and Clubfoot
… and two null alleles in eight genes (CYP1A1, CYP1A2, CYP1B1, CYP2A6, EPHX1, NAT2, GSTM1 and GSTT1) were genotyped in a dataset composed of nonHispanic white and Hispanic multiplex and simplex families. Only one SNP in CYP1A1, rs1048943, had significantly altered transmission in the aggregate …
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Effect of rutaecarpine on caffeine pharmacokinetics in rats
… 3 hours after oral rutaecarpine administration, CYP1A2 activity in the liver tissue is increased by almost 3-fold compared to control rats and highest activity (9-fold compared to control) is found in the liver of rats administered with daily oral dose of rutaecarpine, for seven days. A …
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Effect of Mesoporous Silica-Loaded Anticancer Drugs on 3D vs 2D Models of Colon Cancer Cells
… expression of CYP enzymes such as CYP1A1, CYP1A2 and CYP1B1 in 3D spheroids than in 2D monolayer cells (p = 0.0069, p = 0.00001, and p = 0.0004, respectively). Treatment with DMU121MSN (p < 0.001) and OXAMSN (p < 0.01) increased CYP1A1, CYP1A2, and CYP1B1 expression in both 2D and 3D …
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Effect of obesity on hepatic drug metabolism
… to examine the effect of childhood obesity on CYP1A2, CYP2D6, CYP3A4, xanthine oxidase, and NAT2 activity using caffeine and dextromethorphan as probe drugs. Our results conclusively indicate that obesity results in an elevation of xanthine oxidase and NAT2 enzyme activities in obese children …
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Overexpression of Human Aryl Hydrocarbon Receptor in <i> E.coli</i> Using Two Different Solubility Enhancing Tags
… of various genes such as CYP1A1 and CYP1A2 by AhR-ARNT heterodimer. Various cancers have altered levels of AhR in the absence of ligand. Our current knowledge is only limited in the regulation of AhR protein levels in its ligand bound state. However, the mechanism involved in the …
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From iPSCs to Engineered Heart and Liver Models: Modulating Genetic and Extracellular State for Maturity
… significantly improved albumin secretion and CYP1A2 metabolism across donors. In parallel, we evaluated extracellular matrix (ECM) biology in hepatic differentiation, finding that defined ECM proteins, decellularized liver ECM, and electrospun natural polymer nanofibers, substantially enhanced …
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Genetically engineering a new system for the expression of cytochrome P450 enzymes in insect cells using novel P450 reductases
… of seven CYPs, CYP2D6, CYP3A4, CYP1A1, CYP1B1, CYP1A2, CYP2E1 and CYP2C8 in conjunction with different CPR species (the native human CPR, variants of human CPR and the yeast CPR) using the baculovirus expression system. In my studies I have found that different CPRs have different coupling …
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Effects of Pycnogenol on Microsomal Cytochrome P450 Activity and Apoptosis
… Western blot analysis of expressed CYP2B1 and CYP1A2 protein in lung and liver microsomes from pycnogenol-treated rats did not correlate with the effects of O-dealkylation in these rats.</p> <p>The effect of pycnogenol on apoptosis in cultured "normal" human mammary (MCF-10) cells and human …
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Identification de co-régulateurs impliqués dans la réponse transcriptionnelle induite par les récepteurs AhR et ER[alpha]
… gènes cibles de AhR à savoir les gènes CYP1A1, CYP1A2, CYP1B1, suite au traitement avec le TCDD. Le niveau d'induction du gène CYP1A1 diminue alors que celui du gène CYP1B1 reste constant. Cela diminuerait le ratio CYP1A1/CYP1B1 et ferait augmenter le risque pour le cancer. En effet, CYP1A1 …
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Farnesol-Mediated Regulation Of Hepatic Lipid Metabolism In Heparg Cells
… enzymes, such as CYP3A4, CYP2B6, CYP1A2 and CYP2E1 were also attenuated by co-treatment with farnesol. Our findings show for the first time that farnesol regulates human hepatic lipid metabolism and suppresses lipid accumulation in HepaRG cells under steatogenic conditions by …
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