The Combination of Electrochemistry and Microfluidic Technology in Drug Metabolism Studies
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DOI: 10.1002/open.202200100
Abstract: Abstract Drugs are metabolized within the liver (pH 7.4) by phase I and phase II metabolism. During the process, reactive metabolites can be formed that react covalently with biomolecules and induce toxicity. Identifying and detecting reactive… read more here.
Keywords: drug metabolism; electrochemistry microfluidic; electrochemistry; drug ... See more keywords
Transcriptional and post-transcriptional regulation of the pregnane X receptor: a rationale for interindividual variability in drug metabolism
Sign Up to like & getrecommendations! Published in 2020 at "Archives of Toxicology"
DOI: 10.1007/s00204-020-02916-x
Abstract: The pregnane X receptor (PXR, encoded by the NR1I2 gene) is a ligand-regulated transcription factor originally described as a master regulator of xenobiotic detoxification. Later, however, PXR was also shown to interact with endogenous metabolism… read more here.
Keywords: pxr expression; expression; drug metabolism; regulation ... See more keywords
Digital microfluidic immobilized cytochrome P450 reactors with integrated inkjet-printed microheaters for droplet-based drug metabolism research
Sign Up to like & getrecommendations! Published in 2018 at "Analytical and Bioanalytical Chemistry"
DOI: 10.1007/s00216-018-1280-7
Abstract: We report the development and characterization of digital microfluidic (DMF) immobilized enzyme reactors (IMERs) for studying cytochrome P450 (CYP)-mediated drug metabolism on droplet scale. The on-chip IMERs consist of porous polymer (thiol-ene) monolith plugs prepared… read more here.
Keywords: inkjet printed; droplet based; digital microfluidic; printed microheaters ... See more keywords
In vitro Phase I- and Phase II-Drug Metabolism in The Liver of Juvenile and Adult Göttingen Minipigs
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DOI: 10.1007/s11095-017-2101-y
Abstract: PurposeIn view of pediatric drug development, juvenile animal studies are gaining importance. However, data on drug metabolizing capacities of juvenile animals are scarce, especially in non-rodent species. Therefore, we aimed to characterize the in vitro… read more here.
Keywords: adult; drug; day; drug metabolism ... See more keywords
The influence of genetic polymorphisms in drug metabolism enzymes and transporters on the pharmacokinetics of different fluvastatin formulations
Sign Up to like & getrecommendations! Published in 2020 at "Asian Journal of Pharmaceutical Sciences"
DOI: 10.1016/j.ajps.2019.06.002
Abstract: The purpose of the present study was to investigate the impact of genetic polymorphism on fluvastatin pharmacokinetics. In addition, we compared the fluvastatin pharmacokinetics differences between extended-release (ER) 80 mg tablet and immediate-release (IR) 40 mg capsule… read more here.
Keywords: genetic polymorphisms; drug metabolism; fluvastatin; slco1b1 ... See more keywords
Personalized Mapping of Drug Metabolism by the Human Gut Microbiome
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DOI: 10.1016/j.cell.2020.05.001
Abstract: The human gut microbiome harbors hundreds of bacterial species with diverse biochemical capabilities. Dozens of drugs have been shown to be metabolized by single isolates from the gut microbiome, but the extent of this phenomenon… read more here.
Keywords: microbiome; human gut; drug metabolism; gut microbiome ... See more keywords
Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective.
Sign Up to like & getrecommendations! Published in 2020 at "Drug discovery today"
DOI: 10.1016/j.drudis.2020.07.013
Abstract: Proteolysis-targeting chimeras (PROTACs) are an emerging therapeutic modality with the potential to open target space not accessible to conventional small molecules via a degradation-based mechanism; however, their bifunctional nature can result in physicochemical properties that… read more here.
Keywords: metabolism pharmacokinetics; targeting chimeras; drug; proteolysis targeting ... See more keywords
Elevated bilirubin, alkaline phosphatase at onset, and drug metabolism are associated with prolonged recovery from DILI.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of hepatology"
DOI: 10.1016/j.jhep.2021.03.021
Abstract: BACKGROUND & AIMS Although most drug-induced liver injury (DILI) cases resolve after the culprit medication is discontinued, time to recovery varies among patients, with 6-12% developing a chronic disease. Here, we investigated clinical factors and… read more here.
Keywords: recovery; time; drug; model ... See more keywords
Intrauterine growth restriction may reduce hepatic drug metabolism in the early neonatal period
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DOI: 10.1016/j.phrs.2018.06.003
Abstract: Graphical abstract Figure. No caption available. &NA; The effects of intrauterine growth restriction (IUGR) extend well into postnatal life. IUGR is associated with an increased risk of adverse health outcomes, which often leads to greater… read more here.
Keywords: drug; intrauterine growth; iugr; hepatic drug ... See more keywords
Investigation of nonalcoholic fatty liver disease‐induced drug metabolism by comparative global toxicoproteomics
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DOI: 10.1016/j.taap.2018.05.021
Abstract: &NA; Non‐alcoholic fatty liver disease (NAFLD) includes conditions such as steatosis, non‐alcoholic steatohepatitis, and ultimately hepatocellular carcinoma. Although the pathology of NAFLD is well‐established, NAFLD‐induced drug metabolism mediated by cytochrome P450 (CYP) in the liver… read more here.
Keywords: fatty liver; induced drug; drug; liver disease ... See more keywords
Real-Time Monitoring of Host-Gut Microbial Interspecies Interaction in Anticancer Drug Metabolism.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.1c10998
Abstract: Gut microbiome can affect drug metabolism considerably, leading to modified drug response. However, quantitative estimation of host vs. microbial contributions in a living host-gut microbiome system has been challenging. Using the interspecies system of Caenorhabditis… read more here.
Keywords: metabolism; host gut; drug metabolism; real time ... See more keywords