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Artykuły w czasopismach na temat "Human liver microsomes"

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Minoda, Yuko, and Evan D. Kharasch. "Halothane-dependent Lipid Peroxidation in Human Liver Microsomes Is Catalyzed by Cytochrome P4502A6 (CYP2A6)." Anesthesiology 95, no. 2 (August 1, 2001): 509–14. http://dx.doi.org/10.1097/00000542-200108000-00037.

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Background Halothane is extensively (approximately 50%) metabolized in humans and undergoes both oxidative and reductive cytochrome P450-catalyzed hepatic biotransformation. Halothane is reduced under low oxygen tensions by CYP2A6 and CYP3A4 in human liver microsome to an unstable free radical, and then to the volatile metabolites chlorodifluoroethene (CDE) and chlorotrifluoroethane (CTE). The free radical is also thought to initiate lipid peroxidation. Halothane-dependent lipid peroxidation has been shown in animals in vitro and in vivo but has not been evaluated in humans. This investigation
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Myllynen, P., P. Pienimäki, H. Raunio, and K. Vähäkangas. "Microsomal metabolism of carbamazepine and oxcarbazepine in liver and placenta." Human & Experimental Toxicology 17, no. 12 (December 1998): 668–76. http://dx.doi.org/10.1177/096032719801701204.

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Metabolism of both carbamazepine (CBZ) and oxcarbaze-pine (OCBZ) were catalyzed by human liver microsomes and microsomes from livers of CBZ-induced or non-induced C57BL/6 mice. Human placental microsomes metabolized only OCBZ. Mouse liver microsomes metabolized CBZ to carbamazepine-10,11-epoxide (CBZ-E), 10- hydroxy-10,11-dihydro-carbamazepine (10-OH-CBZ), 3- hydroxy-carbamazepine (3-OH-CBZ), 10,11-trans-dihydroxy-10,11-dihydro-carbamazepine (10,11-D) and to an unidentified metabolite. CBZ-pretreatment of mice increased both ethoxyresorufin O-deethylase activity in the liver and the amount of
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Barnes, T. S., M. D. Burke, and W. T. Melvin. "Differences in adult and foetal human cytochrome P-450 forms recognized by monoclonal antibodies with specificity for the P450III family." Biochemical Journal 260, no. 3 (June 15, 1989): 635–40. http://dx.doi.org/10.1042/bj2600635.

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Six murine monoclonal antibodies raised against a major human adult liver cytochrome P-450 (P-450) of the PCN family (P450III) detected a protein in human foetal liver microsomes (microsomal fractions) which had an approx. 1 kDa higher molecular mass on SDS/polyacrylamide-gel electrophoresis than the protein recognized in human adult liver microsomes. Although each of the antibodies recognized both the adult and the foetal forms, antibody HL4 showed higher affinity for the foetal form. Recognition by the monoclonal antibodies of peptides generated by proteolytic cleavage of microsomal proteins
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George, R., P. J. Davis, L. Luong, and M. J. Poznansky. "Cholesterol-mediated regulation of HMG-CoA reductase in microsomes from human skin fibroblasts and rat liver." Biochemistry and Cell Biology 68, no. 3 (March 1, 1990): 674–79. http://dx.doi.org/10.1139/o90-097.

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3-Hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase activity was determined in microsomes from human skin fibroblasts and rat liver that had been variously manipulated in vivo or in tissue culture to up- and down-regulate the enzyme. The cholesterol content of these microsomal preparations was then altered by depletion to or enrichment from either cholesterol-free or cholesterol-rich lipid vesicles. Microsomes from human skin fibroblasts responded to cholesterol depletion by increasing HMG-CoA reductase activity and by decreasing it in response to cholesterol enrichment. This was independent of
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Nguyen, Ngoc, Ngoc Cao, Thi Nguyen, Thien-Kim Le, Gun Cha, Soo-Keun Choi, Jae-Gu Pan, Soo-Jin Yeom, Hyung-Sik Kang, and Chul-Ho Yun. "Regioselective Hydroxylation of Phloretin, a Bioactive Compound from Apples, by Human Cytochrome P450 Enzymes." Pharmaceuticals 13, no. 11 (October 22, 2020): 330. http://dx.doi.org/10.3390/ph13110330.

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Phloretin, the major polyphenol compound in apples and apple products, is interesting because it shows beneficial effects on human health. It is mainly found as a form of glucoside, phlorizin. However, the metabolic pathway of phloretin in humans has not been reported. Therefore, identifying phloretin metabolites made in human liver microsomes and the human cytochrome P450 (P450) enzymes to make them is interesting. In this study, the roles of human liver P450s for phloretin oxidation were examined using human liver microsomes and recombinant human liver P450s. One major metabolite of phloreti
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Court, Michael H., Su X. Duan, Leah M. Hesse, Karthik Venkatakrishnan, and David J. Greenblatt. "Cytochrome P-450 2B6 Is Responsible for Interindividual Variability of Propofol Hydroxylation by Human Liver Microsomes." Anesthesiology 94, no. 1 (January 1, 2001): 110–19. http://dx.doi.org/10.1097/00000542-200101000-00021.

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Background Oxidation of propofol to 4-hydroxypropofol represents a significant pathway in the metabolism of this anesthetic agent in humans. The aim of this study was to identify the principal cytochrome P-450 (CYP) isoforms mediating this biotransformation. Methods Propofol hydroxylation activities and enzyme kinetics were determined using human liver microsomes and cDNA-expressed CYPs. CYP-specific marker activities and CYP2B6 protein content were also quantified in hepatic microsomes for correlational analyses. Finally, inhibitory antibodies were used to ascertain the relative contribution
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Milewich, L., P. C. MacDonald та B. R. Carr. "Activity of 17β-hydroxysteroid oxidoreductase in tissues of the human fetus". Journal of Endocrinology 123, № 3 (грудень 1989): 509–18. http://dx.doi.org/10.1677/joe.0.1230509.

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ABSTRACT The interconversion of oestrone and oestradiol, androstenedione and testosterone, and dehydroepi-androsterone and 5-androstene-3β,17β-diol in mammalian tissues is catalysed by 17β-hydroxysteroid oxidoreductase (17β-HSOR). To identify tissue sites of 17β-HSOR activity in the human fetus, microsomal fractions from 15 different fetal tissues obtained from first and second trimester pregnancies were used for evaluation of enzymatic activity by use of [17α-3H] oestradiol as the substrate and NADP+ as the co-factor. With these reagents, the enzyme-catalysed reaction led to the production of
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Wang, Li, Zhe Wang, Meng-ming Xia, Ying-ying Wang, Hai-yun Wang, and Guo-xin Hu. "Inhibitory effect of silybin on pharmacokinetics of imatinib in vivo and in vitro." Canadian Journal of Physiology and Pharmacology 92, no. 11 (November 2014): 961–64. http://dx.doi.org/10.1139/cjpp-2014-0260.

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The objective of this work was to investigate the effect of orally administered silybin on the pharmacokinetics of imatinib in rats and the metabolism of imatinib in human liver microsome and rat liver microsomes. Eighteen healthy male SD rats were randomly divided into 3 groups: group A (control group), group B (received multiple doses of 50 mg·kg−1 silybin for 15 consecutive days), and group C (received a single dose of 50 mg·kg−1 silybin). A single dose of imatinib was administered orally 30 min after administration of silybin (50 mg·kg−1). Imatinib plasma levels were measured by UPLC-MS/MS
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Senler, T. I., W. L. Dean, L. F. Murray, and J. L. Wittliff. "Quantification of cytochrome P-450-dependent cyclohexane hydroxylase activity in normal and neoplastic reproductive tissues." Biochemical Journal 227, no. 2 (April 15, 1985): 379–87. http://dx.doi.org/10.1042/bj2270379.

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It is well established that liver microsomal cytochrome P-450 participates in steroid metabolism and probably also in the metabolism of anti-oestrogens such as tamoxifen (Nolvadex). Thus it is possible that variations in cytochrome P-450 levels may influence the responsiveness of human breast and endometrial carcinomas to endocrine therapy. Therefore a simple sensitive spectrophotometric assay for determining levels of cytochrome P-450-dependent cyclohexane hydroxylation activity in breast and uterine microsomes (microsomal fractions) has been developed. Cyclohexane was chosen as a substrate b
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Svobodová, Martina, Markéta Martínková, Eva Frei, and Marie Stiborová. "Identification of human enzymes oxidizing a human metabolite of carcinogenic 2-nitroanisole, 2-nitrophenol. Evidence for its oxidative detoxification by human cytochromes P450." Collection of Czechoslovak Chemical Communications 75, no. 6 (2010): 703–19. http://dx.doi.org/10.1135/cccc2010023.

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2-Nitrophenol (2-NP) is the major detoxification metabolite of an important industrial pollutant and a potent carcinogen, 2-nitroanisole (2-NA). Here, we characterized the product of 2-NP metabolism catalyzed by human, rat, rabbit and mouse hepatic microsomes containing cytochromes P450 (CYPs) and identified the major human CYP enzymes participating in this process. The 2-NP metabolite was characterized by mass spectrometry and co-chromatography on HPLC with a synthetic standard, 2,5-dihydroxynitrobenzene (2,5-DNB) to be 2,5-DNB. No nitroreductive metabolism leading to the formation of N-(2-hy
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Rozprawy doktorskie na temat "Human liver microsomes"

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Emery, Maurice George. "Aspects of human CYP 2E1 regulation in health and disease /." Thesis, Connect to this title online; UW restricted, 1999. http://hdl.handle.net/1773/7943.

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McLure, James Alexander, and james mclure@flinders edu au. "Physicochemical determinants of the non-specific binding of drugs to human liver microsomes." Flinders University. Medicine, 2008. http://catalogue.flinders.edu.au./local/adt/public/adt-SFU20081102.165952.

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Accurate determination of the in vitro kinetic parameters Km (Michaelis constant) and Ki (inhibition constant) is critical for the quantitative prediction of in vivo drug clearance and the magnitude of inhibitory drug interactions. A cause of inaccuracy in vitro arises from the assumption that all drug added to an incubation mixture is available for metabolism or inhibition. Many drugs bind non-specifically to the membrane of the in vitro enzyme source. The aims of this thesis were to: 1) investigate the comparative importance of lipophilicity (as log P), and pKa as determinants of the non-sp
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Schjølberg, Tiril Helgesen. "In Vitro Synthesis of Metabolites of three Anabolic Androgenic Steroids, by Human Liver Microsomes." Thesis, Norges teknisk-naturvitenskapelige universitet, Institutt for bioteknologi, 2013. http://urn.kb.se/resolve?urn=urn:nbn:no:ntnu:diva-22910.

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Anabolic androgenic steroids are substances frequently misused to improve physicalperformance in sports. To reveal substances misused as doping, athlete urinesamples are collected and tested. To identify the steroid and/or its metabolitesin urine, reference compounds must exist for comparison. The time-consumingand ethical concerns about in vivo excretion studies for the examination of thesecompounds, make the use of liver fragment microsomes an attractive alternative.The aim of this thesis was to synthesize and identify metabolites from known andrare anabolic androgenic steroids, by the use o
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Maley, Mary. "The role of individual forms of cytochrome P450 in drug metabolism in human liver microsomes." Thesis, University of Aberdeen, 1996. http://digitool.abdn.ac.uk/R?func=search-advanced-go&find_code1=WSN&request1=AAIU078654.

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Human liver microsomal metabolism of nicardipine was investigated and compared to that of another dihydropyridine, felodipine, and to published results for other compounds belonging to this class of drugs. The metabolism of tamoxifen and two iododerivatives, idoxifene and 4-iodotamoxifen, were also investigated. Nicardipine metabolism by human liver microsomes was dissimilar to that of other dihydropyridines in several respects. For most dihydropyridines studied to date, conversion to the corresponding pyridine is the major metabolic pathway; the results from this study suggested that pyridine
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Abu-Omar, Ghada M. "Drug interactions and metabolism of cyclosporin A and steroids by human liver microsomes in vitro." Thesis, University of Aberdeen, 1992. http://digitool.abdn.ac.uk/R?func=search-advanced-go&find_code1=WSN&request1=AAIU545502.

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1) The purpose of this work is to study the enzymology of cyclosporin A (CsA) metabolism by human liver in vitro , in particular investigating the basis for interindividual variations and drug interactions involving CsA metabolism, and to apply this knowledge to the development of a non-invasive test for predicting an individual's ability to metabolise CsA in vivo . The ultimate aim is to help to improve CsA therapy by understanding the factors which determine its metabolism in patients. 2) Human liver microsomes metabolised cyclosporin A (Km 25M) to eight identifiable metabolites, which were
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Dowsley, Taylor Forbes. "CYP2E1-dependent bioactivation of 1,1-dichloroethylene to reactive intermediates in murine and human lung and liver microsomes." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1999. http://www.collectionscanada.ca/obj/s4/f2/dsk2/ftp02/NQ38304.pdf.

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Strömqvist, Malin. "Development of quantitative methods for the determination of vemurafenib and its metabolites in human plasma." Thesis, Linköpings universitet, Kemi, 2014. http://urn.kb.se/resolve?urn=urn:nbn:se:liu:diva-110076.

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Vemurafenib is a potent serine/threonine kinase inhibitor and is registered as Zelboraf® for the treatment of metastatic melanomas harboring BRAFV600E mutations. There is a large individual variation in drug response and the side effects observed among patients treated with Zelboraf® has proven to be severe.  LC-MS/MS methods were developed to measure vemurafenib and its metabolites in human plasma for prediction of treatment outcome and side effects in order to individualize treatment with Zelboraf®.  A novel, rapid quantification method was developed for vemurafenib using a stable isotope la
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Shepard, Dale Randall. "The Metabolism of Phenytoin by Human Liver Microsomes and Cytochrome P450s Expressed in Saccharomyces Cerevisiae and COS-1 Cells /." The Ohio State University, 1995. http://rave.ohiolink.edu/etdc/view?acc_num=osu1487931512618872.

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Uwimana, Eric. "Probing the PCB metabolome: metabolism of chiral and non-chiral polychlorinated biphenyls to chiral hydroxylated metabolites in humans and rats." Diss., University of Iowa, 2018. https://ir.uiowa.edu/etd/6657.

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Polychlorinated biphenyls (PCBs) continue to pose a health concern because of their predominance in the diet and air as well as in environmental samples and humans. PCB congeners with 3 or 4 chlorine substituents in ortho position have been associated with neurodevelopmental disorders. Hydroxylated metabolites (OH-PCBs) of these PCBs are also potentially toxic to the developing brain. Metabolism studies have mainly focused on animal models. However, preliminary data from this dissertation work have revealed PCB metabolism differences between laboratory animal models and humans in terms of meta
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Larabi, Islam Amine. "Nouveaux produits de synthèse : analyse, consommation et métabolisme ; Applications cliniques et médicolégales Rapid and simultaneous screening of new psychoactive substances and conventional drugs of abuse. A comparative study of Biochip Array Technology versus LC-MS/MS in whole blood and urine Development of a sensitive untargeted liquid chromatography– high resolution mass spectrometry screening devoted to hair analysis through a shared MS2 spectra database: A step toward early detection of new psychoactive substances Validation of an UPLC-MS/MS method for the determination of sixteen synthetic cannabinoids in human hair. Application to document chronic use of JWH-122 following a non-fatal overdose Development and validation of liquid chromatography-tandem mass spectrometry targeted screening of 16 fentanyl analogs and U-47700 in hair: Application to 137 authentic samples Prevalence and Surveillance of Synthetic Cathinones Use by Hair Analysis: An Update Review Prevalence of New Psychoactive Substances(NPS) and conventional drugs of abuse (DOA) in high risk populations from Paris(France) and its suburbs A cross sectional study by hair testing(2012–2017) Evaluation of drug abuse by hair analysis and self-reported use among MSM under PrEP: Results from a sub-study of the ANRS-IPERGAY trial. Hair testing for 3‑fluorofentanyl, furanylfentanyl, methoxyacetylfentanyl, carfentanil, acetylfentanyl and fentanyl by LC–MS/MS after unintentional overdose Drug‐facilitated sexual assault (DFSA) involving 4‐methylethcathinone (4‐MEC),3,4‐Methylenedioxypyrovalerone (MDPV), and doxylamine highlighted by hair analysis Metabolic Profiling of Deschloro-N-ethyl-ketamine (O-PCE) and identification of new target metabolites in urine and hair using human liver microsomes and high-resolution accurate mass spectrometry." Thesis, université Paris-Saclay, 2020. http://www.theses.fr/2020UPASL029.

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L’objectif de ce travail a été de développer deux approches analytiques dédiées à l’analyse toxicologique des nouveaux produits de synthèse (NPS) dans différentes matrices biologiques (sang, urine et cheveux). La première est basée sur le criblage non ciblé par chimiluminescence sur biopuces et chromatographie liquide couplée à la spectrométrie de masse haute résolution (LC-HRMS) et la deuxième correspond à un criblage ciblé par spectrométrie de masse en tandem (LC-MS/MS). Ces deux approches ont ensuite été appliquées dans des études observationnelles pour évaluer la consommation de NPS dans d
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Książki na temat "Human liver microsomes"

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Nicotine C-oxidation by human liver microsomes: A major role for CYP2A6. Ottawa: National Library of Canada, 1996.

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Barsoum, Rashad S. Schistosomiasis. Edited by Neil Sheerin. Oxford University Press, 2018. http://dx.doi.org/10.1093/med/9780199592548.003.0181_update_001.

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AbstractSchistosomes are blood flukes that parasitize humans, apes, cattle, and other animals. In these definitive hosts they are bisexual, and lay eggs which are shed to fresh water where they complete an asexual cycle in different snails, ending in the release of cercariae which infect the definitive hosts to complete the life cycle.Seven of over 100 species of schistosomes are human pathogens, causing disease in different organs depending on the parasite species. Racial and genetic factors are involved in susceptibility, severity, and sequelae of infection.Morbidity is induced by the host’s
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Części książek na temat "Human liver microsomes"

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McManus, M. E., D. J. Birkett, W. M. Burgess, I. Stupans, J. A. Koenig, A. R. Boobis, D. S. Davies, P. J. Wirth, P. H. Grantham, and S. S. Thorgeirsson. "Flavin-Containing Monooxygenase Activity in Human Liver Microsomes." In Biological Reactive Intermediates III, 773–79. Boston, MA: Springer US, 1986. http://dx.doi.org/10.1007/978-1-4684-5134-4_72.

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Jia, Jia. "Cytochrome P450 Inhibition Assay Using Human Liver Microsomes." In Methods in Pharmacology and Toxicology, 91–105. New York, NY: Springer US, 2021. http://dx.doi.org/10.1007/978-1-0716-1542-3_6.

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Yan, Zhengyin, and Gary W. Caldwell. "Evaluation of Cytochrome P450 Inhibition in Human Liver Microsomes." In Optimization in Drug Discovery, 231–44. Totowa, NJ: Humana Press, 2004. http://dx.doi.org/10.1385/1-59259-800-5:231.

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Coe, Kevin J., Judith Skaptason, and Tatiana Koudriakova. "Identification of Time-Dependent CYP Inhibitors Using Human Liver Microsomes (HLM)." In Methods in Pharmacology and Toxicology, 305–14. Totowa, NJ: Humana Press, 2013. http://dx.doi.org/10.1007/978-1-62703-742-6_18.

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Wu, Wu-Nan, and Linda A. McKown. "In Vitro Drug Metabolite Profiling Using Hepatic S9 and Human Liver Microsomes." In Optimization in Drug Discovery, 163–84. Totowa, NJ: Humana Press, 2004. http://dx.doi.org/10.1385/1-59259-800-5:163.

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Christians, U., H. M. Schiebel, J. Bleck, and K. Fr Sewing. "Elucidation of the Metabolic Pathways of Cyclosporine in Vitro by Human Liver Microsomes." In Drugs and the Liver: High Risk Patients and Transplantation, 165–70. Dordrecht: Springer Netherlands, 1993. http://dx.doi.org/10.1007/978-94-011-1994-8_27.

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Benga, Gh. "Molecular Composition, Fluidity of Membranes and Functional Properties of Human Liver Mitochondria and Microsomes." In Molecular Basis of Membrane-Associated Diseases, 285–302. Berlin, Heidelberg: Springer Berlin Heidelberg, 1989. http://dx.doi.org/10.1007/978-3-642-74415-0_24.

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Hörnsten, Lena, Johan Bylund, and Ernst H. Oliw. "Bisallylic Hydroxylation of Linoleic and Arachidonic Acids by Adult and Fetal Human Liver Microsomes and a Comparison with Human Recombinant Cytochromes P450." In Advances in Experimental Medicine and Biology, 123–26. Boston, MA: Springer US, 1997. http://dx.doi.org/10.1007/978-1-4899-1810-9_25.

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Caldwell, Gary W., and Zhengyin Yan. "Rapidly Distinguishing Reversible and Time-Dependent CYP450 Inhibition Using Human Liver Microsomes, Co-incubation, and Continuous Fluorometric Kinetic Analyses." In Methods in Pharmacology and Toxicology, 281–303. Totowa, NJ: Humana Press, 2013. http://dx.doi.org/10.1007/978-1-62703-742-6_17.

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Ahmed, S. Sohail, Kimberly L. Napoli, and Henry W. Strobel. "Oxygen Radical Formation Due to the Effect of Varying Hydrogen Ion Concentrations on Cytochrome P450-Catalyzed Cyclosporine Metabolism in Rat and Human Liver Microsomes." In Advances in Experimental Medicine and Biology, 135–39. Boston, MA: Springer US, 1996. http://dx.doi.org/10.1007/978-1-4757-9480-9_19.

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Streszczenia konferencji na temat "Human liver microsomes"

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Widdison, Wayne C., Sharon Wilhelm, Karen Veale, Yelena Kovtun, Hans Erickson, Charlene Audette, Barbara Leeca, Gregory Jones, and Ravi Chari. "Abstract 2668: Detoxification of metabolites from antibody-maytansinoid conjugates by human liver microsomes." In Proceedings: AACR 101st Annual Meeting 2010‐‐ Apr 17‐21, 2010; Washington, DC. American Association for Cancer Research, 2010. http://dx.doi.org/10.1158/1538-7445.am10-2668.

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Liu, Xing, Albert DeJesus, Dana Vardeman, Zhisong Cao, and Beppino Giovanella. "Abstract 4337:In vitrobiotransformation of and inhibitory effects of CZ48 in human liver microsomes." In Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA. American Association for Cancer Research, 2014. http://dx.doi.org/10.1158/1538-7445.am2014-4337.

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Grafakou, M. E., C. Barda, E. Skaltsa, and J. Heilmann. "Identification of parthenolide metabolites in human liver microsomes by LC-Q-TOF-MS/MS." In GA – 69th Annual Meeting 2021, Virtual conference. Georg Thieme Verlag, 2021. http://dx.doi.org/10.1055/s-0041-1736874.

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Ouyang, Hui, Huiping Liao, Junmao Li, Mingzhen He, Yan Li, Xiaoyong Rao, Qi Wang, Shilin Yang, Zhifeng Li, and Yulin Feng. "COMPARATIVE METABOLISM CHARACTERISTICS RESEARCH OF TETRAHYDROPALMATINE IN FIVE SPECIES (DOG, HUMAN, MICE, MONKEY, AND RAT) LIVER MICROSOMES BY UHPLC/ESI-QTOF-MS/MS." In 2016 International Conference on Biotechnology and Medical Science. WORLD SCIENTIFIC, 2016. http://dx.doi.org/10.1142/9789813145870_0023.

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Raporty organizacyjne na temat "Human liver microsomes"

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Abou-Donia, M. B., and A. W. Abu-Quare. In Vitro Metabolism of Pyridostigmine Bromide (PB), DEET and Permethrin, Alone and in Combination by Human Plasma and Liver Microsomes. Fort Belvoir, VA: Defense Technical Information Center, March 2001. http://dx.doi.org/10.21236/ada402080.

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Casabar, Richard C., Andrew D. Wallace, Ernest Hodgson, and Randy L. Rose. Metabolism of Endosulfan-Alpha by Human Liver Microsomes and its Utility as a Simultaneous In Vitro Probe for CYP2B6 and CYP3A4. Fort Belvoir, VA: Defense Technical Information Center, March 2006. http://dx.doi.org/10.21236/ada445178.

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