Academic literature on the topic 'Uridine 5'-diphospho-glucuronosyltransferase (UGT)'

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Journal articles on the topic "Uridine 5'-diphospho-glucuronosyltransferase (UGT)"

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Reddy, Micaela B., Michael B. Bolger, Grace Fraczkiewicz, et al. "PBPK Modeling as a Tool for Predicting and Understanding Intestinal Metabolism of Uridine 5′-Diphospho-glucuronosyltransferase Substrates." Pharmaceutics 13, no. 9 (2021): 1325. http://dx.doi.org/10.3390/pharmaceutics13091325.

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Uridine 5′-diphospho-glucuronosyltransferases (UGTs) are expressed in the small intestines, but prediction of first-pass extraction from the related metabolism is not well studied. This work assesses physiologically based pharmacokinetic (PBPK) modeling as a tool for predicting intestinal metabolism due to UGTs in the human gastrointestinal tract. Available data for intestinal UGT expression levels and in vitro approaches that can be used to predict intestinal metabolism of UGT substrates are reviewed. Human PBPK models for UGT substrates with varying extents of UGT-mediated intestinal metabol
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Cho, Pil, Sanjita Paudel, Doohyun Lee, et al. "Characterization of CYPs and UGTs Involved in Human Liver Microsomal Metabolism of Osthenol." Pharmaceutics 10, no. 3 (2018): 141. http://dx.doi.org/10.3390/pharmaceutics10030141.

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Osthenol is a prenylated coumarin isolated from the root of Angelica koreana and Angelica dahurica, and is an O-demethylated metabolite of osthole in vivo. Its various pharmacological effects have been reported previously. The metabolic pathway of osthenol was partially confirmed in rat osthole studies, and 11 metabolic products were identified in rat urine. However, the metabolic pathway of osthenol in human liver microsomes (HLM) has not been reported. In this study, we elucidated the structure of generated metabolites using a high-resolution quadrupole-orbitrap mass spectrometer (HR-MS/MS)
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Trapnell, Carol Braun, Raymond W. Klecker, Carlos Jamis-Dow, and Jerry M. Collins. "Glucuronidation of 3′-Azido-3′-Deoxythymidine (Zidovudine) by Human Liver Microsomes: Relevance to Clinical Pharmacokinetic Interactions with Atovaquone, Fluconazole, Methadone, and Valproic Acid." Antimicrobial Agents and Chemotherapy 42, no. 7 (1998): 1592–96. http://dx.doi.org/10.1128/aac.42.7.1592.

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ABSTRACT Zidovudine (3′-azido-3′-deoxythymidine [AZT]), an antiviral nucleoside analog effective in the treatment of human immunodeficiency virus infection, is primarily metabolized to an inactive glucuronide form, GAZT, via uridine-5′-diphospho-glucuronosyltransferase (UGT) enzymes. UGT enzymes exist as different isoforms, each exhibiting substrate specificity. Published clinical studies have shown that atovaquone, fluconazole, methadone, and valproic acid decreased GAZT formation, presumably due to UGT inhibition. The effect of these drugs on AZT glucuronidation was assessed in vitro by usin
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Park, Ria, Eun Jeong Park, Yong-Yeon Cho, et al. "Tetrahydrofurofuranoid Lignans, Eudesmin, Fargesin, Epimagnolin A, Magnolin, and Yangambin Inhibit UDP-Glucuronosyltransferase 1A1 and 1A3 Activities in Human Liver Microsomes." Pharmaceutics 13, no. 2 (2021): 187. http://dx.doi.org/10.3390/pharmaceutics13020187.

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Eudesmin, fargesin, epimagnolin A, magnolin, and yangambin are tetrahydrofurofuranoid lignans with various pharmacological activities found in Magnoliae Flos. The inhibition potencies of eudesmin, fargesin, epimagnolin A, magnolin, and yangambin on six major human uridine 5′-diphospho-glucuronosyltransferase (UGT) activities in human liver microsomes were evaluated using liquid chromatography–tandem mass spectrometry and cocktail substrates. Eudesmin, fargesin, epimagnolin A, magnolin, and yangambin inhibited UGT1A1 and UGT1A3 activities, but showed negligible inhibition of UGT1A4, UGT16, UGT1
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Sawyer, M. B., S. Damaraju, E. Pituskin, et al. "Uridine glucuronosyltransferase 2B7 pharmacogenetics predicts epirubicin clearance and myelosuppression." Journal of Clinical Oncology 27, no. 15_suppl (2009): 2504. http://dx.doi.org/10.1200/jco.2009.27.15_suppl.2504.

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2504 Background: Epirubicin (EPI) is widely used to treat breast cancer. EPI is predominantly metabolized by uridine glucuronosyltransferase (UGT) 2B7 to inactive glucuronides. We previously showed that a UGT enhancer single nucleotide polymorphism (SNP) at position -161 T to C correlated with rates of morphine glucuronidation. Methods: We performed a prospective pharmacogenetic study of effects of this SNP on EPI metabolism in M0 breast cancer patients (PTS) receiving adjuvant or neoadjuvant FEC100 (5-fluorouracil 500 mg/m2, EPI 100 mg/m2 and cyclophosphamide 500 mg/m2) given every 3 wks. PTS
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Choi, Won-Gu, Ria Park, Dong Kyun Kim, Yongho Shin, Yong-Yeon Cho, and Hye Suk Lee. "Mertansine Inhibits mRNA Expression and Enzyme Activities of Cytochrome P450s and Uridine 5′-Diphospho-Glucuronosyltransferases in Human Hepatocytes and Liver Microsomes." Pharmaceutics 12, no. 3 (2020): 220. http://dx.doi.org/10.3390/pharmaceutics12030220.

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Mertansine, a tubulin inhibitor, is used as the cytotoxic component of antibody–drug conjugates (ADCs) for cancer therapy. The effects of mertansine on uridine 5′-diphospho-glucuronosyltransferase (UGT) activities in human liver microsomes and its effects on the mRNA expression of cytochrome P450s (CYPs) and UGTs in human hepatocytes were evaluated to assess the potential for drug–drug interactions (DDIs). Mertansine potently inhibited UGT1A1-catalyzed SN-38 glucuronidation, UGT1A3-catalyzed chenodeoxycholic acid 24-acyl-β-glucuronidation, and UGT1A4-catalyzed trifluoperazine N-β-d-glucuronida
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Bomann, Werner, Helen Tinwell, Peter Jenkinson, and Felix M. Kluxen. "Metribuzin-induced non-adverse liver changes result in rodent-specific non-adverse thyroid effects via uridine 5′-diphospho-glucuronosyltransferase (UDPGT, UGT) modulation." Regulatory Toxicology and Pharmacology 122 (June 2021): 104884. http://dx.doi.org/10.1016/j.yrtph.2021.104884.

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Bomann, W. H., H. Tinwell, and F. Kluxen. "Metribuzin-induced non-adverse liver changes result in rodent-specific non-adverse thyroid effects via Uridine 5'-diphospho-glucuronosyltransferase (UDPGT, UGT) modulation." Toxicology Letters 350 (September 2021): S226. http://dx.doi.org/10.1016/s0378-4274(21)00765-7.

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Reid, Anna-Mari, Risto Juvonen, Pasi Huuskonen, Marko Lehtonen, Markku Pasanen, and Namrita Lall. "In Vitro Human Metabolism and Inhibition Potency of Verbascoside for CYP Enzymes." Molecules 24, no. 11 (2019): 2191. http://dx.doi.org/10.3390/molecules24112191.

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Verbascoside is found in many medicinal plant families such as Verbenaceae. Important biological activities have been ascribed to verbascoside. Investigated in this study is the potential of verbascoside as an adjuvant during tuberculosis treatment. The present study reports on the in vitro metabolism in human hepatic microsomes and cytosol incubations as well as the presence and quantity of verbascoside within Lippia scaberrima. Additionally, studied are the inhibitory properties on human hepatic CYP enzymes together with antioxidant and cytotoxic properties. The results yielded no metabolite
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Naydenova, Zlatina G., Konstantin C. Grancharov, Dimitar K. Alargov, et al. "Inhibition of UDP-glucuronosyltransferase by 5'-O-amino Acid and Oligopeptide Derivatives of Uridine: Structure-Activity Relationships." Zeitschrift für Naturforschung C 53, no. 3-4 (1998): 173–81. http://dx.doi.org/10.1515/znc-1998-3-406.

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Abstract The inhibitory effect of a series of 5′-O-amino acid and oligopeptide derivatives of uridine on rat liver UDP-glucuronosyltransferase (UGT) activities was investigated using two assay systems. A quantitative structure-activity relationship (QSAR) study was performed. The compounds include a lipophilic residue linked to the nucleoside by a variable spacer. More­ over, half of the derivatives have two spacers linked to the uridine moiety. Compound 1, a serine derivative of isopropylideneuridine, was found to be the most potent inhibitor of both 4-nitrophenol (4-NP) and phenolphthalein (
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Dissertations / Theses on the topic "Uridine 5'-diphospho-glucuronosyltransferase (UGT)"

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Leclerc, François. "Évaluation de l'impact des xénobiotiques alimentaires sur la santé materno-foetale : rôle du Bisphénol A." Mémoire, Université de Sherbrooke, 2013. http://hdl.handle.net/11143/6332.

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Au quotidien, nous sommes exposés à une multitude de xénobiotiques, des molécules exogènes à un organisme vivant et qui sont considérées toxiques pour ce dernier. Parmi tous ces xénobiotiques, le Bisphénol-A (BPA), un xénoestrogène, est l'un de ceux attirants le plus l'attention de la communauté scientifique. Des travaux effectués antérieurement par notre laboratoire ont mis en évidence des effets cytotoxiques sur les cellules placentaires (Benachour et Aris, 2009). À de très faibles concentrations, le BPA induit une augmentation significative de l'apoptose et de la nécrose des cytotrophoblast
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Book chapters on the topic "Uridine 5'-diphospho-glucuronosyltransferase (UGT)"

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Sandson, Neil B. "Uridine 5′-diphospho-glucuronoslytransferases (UGTs): Conjugating Cousins." In A Case Approach to Perioperative Drug-Drug Interactions. Springer New York, 2015. http://dx.doi.org/10.1007/978-1-4614-7495-1_12.

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