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Cytochrome P450

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https://www.readbyqxmd.com/read/28346810/an-automated-multiplexed-hepatotoxicity-and-cyp-induction-assay-using-heparg-cells-in-2d-and-3d
#1
Lindsey M Ott, Karthik Ramachandran, Lisa Stehno-Bittel
Drug-induced liver injury (DILI) and drug-drug interactions (DDIs) are concerns when developing safe and efficacious compounds. We have developed an automated multiplex assay to detect hepatotoxicity (i.e., ATP depletion) and metabolism (i.e., cytochrome P450 1A [CYP1A] and cytochrome P450 3A4 [CYP3A4] enzyme activity) in two-dimensional (2D) and three-dimensional (3D) cell cultures. HepaRG cells were cultured in our proprietary micromold plates and produced spheroids. HepaRG cells, in 2D or 3D, expressed liver-specific proteins throughout the culture period, although 3D cultures consistently exhibited higher albumin secretion and CYP1A/CYP3A4 enzyme activity than 2D cultures...
March 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28346781/metabolism-of-ibuprofen-by-phragmites-australis-uptake-and-phytodegradation
#2
Yujie He, Alette A M Langenhoff, Nora B Sutton, Huub H M Rijnaarts, Marco H Blokland, Feiran Chen, Christian Huber, Peter Schröder
This study explores ibuprofen (IBP) uptake and transformation in the wetland plant species Phragmites australis and the underlying mechanisms. We grew P. australis in perlite under greenhouse conditions and treated plants with 60 µg/l of IBP. Roots and rhizomes (RR), stems and leaves (SL), and liquid samples were collected during 21 days of exposure. Results show that P. australis can take up, translocate, and degrade IBP. IBP was completely removed from the liquid medium after 21 days with a half-life of 2...
March 27, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28345956/modulation-of-steroidogenesis-by-vitamin-d3-in-granulosa-cells-of-the-mouse-model-of-polycystic-ovarian-syndrome
#3
Shabnam Bakhshalizadeh, Fardin Amidi, Ashraf Alleyassin, Masoud Soleimani, Reza Shirazi, Maryam Shabani Nashtaei
Polycystic ovarian syndrome (PCOS) is the most common endocrine disorder of women of reproductive age characterized by polycystic ovarian morphology, anovulation or oligomenorrhea, and hyperandrogenism. It is shown that disruption in the steroidogenesis pathway caused by excess androgen in PCOS is a critical element of abnormal folliculogenesis and failure in dominant follicle selection. Vitamin D plays an important role in the regulation of ovulatory dysfunction and can influence genes involved in steroidogenesis in granulosa cells...
March 27, 2017: Systems Biology in Reproductive Medicine
https://www.readbyqxmd.com/read/28345676/bioconversion-of-stilbenes-in-genetically-engineered-root-and-cell-cultures-of-tobacco
#4
Diego Hidalgo, Ascensión Martínez-Márquez, Elisabeth Moyano, Roque Bru-Martínez, Purificación Corchete, Javier Palazon
It is currently possible to transfer a biosynthetic pathway from a plant to another organism. This system has been exploited to transfer the metabolic richness of certain plant species to other plants or even to more simple metabolic organisms such as yeast or bacteria for the production of high added value plant compounds. Another application is to bioconvert substrates into scarcer or biologically more interesting compounds, such as piceatannol and pterostilbene. These two resveratrol-derived stilbenes, which have very promising pharmacological activities, are found in plants only in small amounts...
March 27, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28345306/the-burden-and-management-of-cytochrome-p450-2d6-cyp2d6-mediated-drug-drug-interaction-ddi-co-medication-of-metoprolol-and-paroxetine-or-fluoxetine-in-the-elderly
#5
Muh Akbar Bahar, Eelko Hak, Jens H J Bos, Sander D Borgsteede, Bob Wilffert
PURPOSE: Metoprolol and paroxetine/fluoxetine are inevitably co-prescribed because cardiovascular disorders and depression often coexist in the elderly. This leads to CYP2D6-mediated drug-drug interactions (DDI). Because systematic evaluations are lacking, we assessed the burden of metoprolol-paroxetine/fluoxetine interaction in the elderly and how these interactions are managed in Dutch community pharmacies. METHOD: Dispensing data were collected from the University of Groningen pharmacy database (IADB...
March 26, 2017: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/28344492/cyp2c9-cypc19-and-cyp2d6-gene-profiles-and-gene-susceptibility-to-drug-response-and-toxicity-in-turkish-population
#6
Merve Arici, Gül Özhan
Pharmacogenetics is a vast field covering drug discovery research, the genetic basis of pharmacokinetics and dynamics, genetic testing and clinical management in diseases. Pharmacogenetic approach usually focuses on variations of drug transporters, drug targets, drug metabolizing enzymes and other biomarker genes. Cytochrome P450 (CYP) enzymes, an essential source of variability in drug-response, play role in not only phase I-dependent metabolism of xenobiotics but also metabolism of endogenous compounds such as steroids, vitamins and fatty acids...
March 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28344482/the-genetic-profiles-of-cyp1a1-cyp1a2-and-cyp2e1-enzymes-as-susceptibility-factor-in-xenobiotic-toxicity-in-turkish-population
#7
Merve Arici, Gül Özhan
Evaluation and sequencing of heritable alterations in the human genome and the large-scale identification of gene polymorphism for understanding the genetic background of individuals in response to potential toxicants are provided by toxicogenetics. Cytochrome P450 (CYP) enzymes play role not only phase I-dependent metabolism of xenobiotics but also metabolism of endogenous compounds. CYP1A1, CYP1A2 and CYP2E1 enzymes, which are in phase I enzymes, are responsible for metabolic activation and detoxification of several chemical compounds...
February 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28344076/inhibition-of-human-cyp3a4-and-cyp3a5-enzymes-by-gomisin-c-and-gomisin-g-two-lignan-analogs-derived-from-schisandra-chinensis
#8
Jin Zhao, Tao Sun, Yun-Feng Cao, Zhong-Ze Fang, Hong-Zhi Sun, Zhi-Tu Zhu, Kun Yang, Yong-Zhe Liu, Frank J Gonzalez, Jing-Jing Wu, Jun Yin
Gomisin C (GC) and gomisin G (GG) are two lignan analogs isolated from the Traditional Chinese Medicine Schisandra chinensis which possesses multiple pharmacological activities. However, the potential herb-drug interactions (HDI) between these lignans and other drugs through inhibiting human cytochrome P450 3A4 (CYP3A4) and CYP3A5 remains unclear. In the present study, the inhibitory action of GC and GG on CYP3A4 and CYP3A5 were investigated. The results demonstrated that both GC and GG strongly inhibited CYP3A-mediated midazolam 1'-hydroxylation, nifedipine oxidation and testosterone 6β-hydroxylation...
March 23, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28343293/pharmacokinetic-and-pharmacodynamic-considerations-in-the-treatment-of-chronic-lymphocytic-leukemia-ibrutinib-idelalisib-and-venetoclax
#9
REVIEW
Madeline Waldron, Allison Winter, Brian T Hill
Management of chronic lymphocytic leukemia has changed markedly over the last several years with the emergence of several novel oral agents targeting B-cell receptor and Bcl-2 signaling pathways. For patients requiring treatment, ibrutinib, idelalisib, and venetoclax offer unique clinical benefits with a different set of therapeutic considerations compared with traditional parenteral therapy. Despite the conveniences afforded by oral therapy, these agents also carry unique logistical obstacles. Drug interactions with agents that are metabolized via the cytochrome P450 3A4 pathway are possible with all three agents...
March 25, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28343019/a-new-opportunity-for-nanomedicines-micellar-cytochrome-p450-inhibitors-to-improve-drug-efficacy-in-a-cancer-therapy-model
#10
Marion Paolini, Laurence Poul, Audrey Darmon, Matthieu Germain, Agnès Pottier, Laurent Levy, Eric Vibert
Nanomedicines are mainly used as drug delivery systems; here we evaluate a new application - to inhibit a drug's metabolism thereby enhancing its effective dose. Micelles containing the natural furanocoumarin 6',7'-dihydroxybergamottin (DHB), a known CYP450 inhibitor, were developed to transiently block hepatic CYP450-mediated drug metabolism and increase the bioavailability of the oncology drug docetaxel. Administered in mice 24hours prior to the drug, DHB-micelles enhanced antitumor efficacy in the tumor xenograft models HT-29 and MDA-MB-231, when compared to the drug alone...
March 22, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/28342136/molecular-basis-of-p450-oletje-an-investigation-of-substrate-binding-mechanism-and-major-pathways
#11
Juan Du, Lin Liu, Li Zhong Guo, Xiao Jun Yao, Jian Ming Yang
Cytochrome P450 OleTJE has attracted much attention for its ability to catalyze the decarboxylation of long chain fatty acids to generate alkenes, which are not only biofuel molecule, but also can be used broadly for making lubricants, polymers and detergents. In this study, the molecular basis of the binding mechanism of P450 OleTJE for arachidic acid, myristic acid, and caprylic acid was investigated by utilizing conventional molecular dynamics simulation and binding free energy calculations. Moreover, random acceleration molecular dynamics (RAMD) simulations were performed to uncover the most probable access/egress channels for different fatty acids...
March 25, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28341216/effects-of-methimazole-on-drosophila-glucolipid-metabolism-in-vitro-and-in-vivo
#12
Qi Wei, Bo Hu, Yuan Xue, David Kibe Mburu, Xian Tao, Jianya Su
Methimazole (MMI) is an antithyroid agent widely used in the treatment of hyperthyroidism, and metabolized by cytochrome P450 enzymes and flavin-containing monooxygenases in mammals. However, drug overdose and the inadequate detoxification of the metabolite(s) are responsible for hepatocellular damage and organ dysfunction. Depending on the desired properties, Drosophila melanogaster has recently emerged as an ideal model organism for the study of human diseases. Here we investigated the changes in metabolic profiles and mRNA expressions related to glucolipid metabolism in response to treatment with MMI in Drosophila...
March 21, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28341215/identification-and-molecular-characterization-of-cytochrome-p450-cyp450-family-genes-in-the-marine-ciliate-euplotes-crassus-the-effect-of-benzo-a-pyrene-and-beta-naphthoflavone
#13
Bora Yim, Hokyun Kim, Jisoo Kim, Haeyeon Kim, Eun-Ji Won, Young-Mi Lee
Marine ciliate Euplotes crassus, a single-cell eukaryote, and has been considered as a model organism for monitoring of environmental pollutions in sediments. Cytochrome P450 (CYP450) monooxygenase are phase I enzyme involved in detoxification of environmental pollutants, such as polycyclic aromatic hydrocarbons (PAHs). However, little information on CYP450 family genes in ciliate is available. In the present study, acute toxicity of PAH, benzo[a]pyrene (B[a]P) and PAH-like model compound, beta-naphthoflavone (β-NF), was investigated; full-length cDNA sequences and genomic structure of five CYP450 genes (CYP5680A1, CYP5681A1, CYP5681B1, CYP5682A1, and CYP5683A1) were analyzed; and finally their activities and transcriptional changes were measured after exposure to PAHs for 48h...
March 21, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28341123/acetaminophen-analog-but-not-reactive-metabolite-induces-cyp3a-activity-via-inhibition-of-protein-degradation
#14
Masataka Santoh, Seigo Sanoh, Yuya Ohtsuki, Yoko Ejiri, Yaichiro Kotake, Shigeru Ohta
Cytochrome P450 (CYP) 3A subfamily members are known to metabolize various types of drugs, highlighting the importance of understanding drug-drug interactions (DDI) depending on CYP3A induction or inhibition. While transcriptional regulation of CYP3A members is widely understood, post-translational regulation needs to be elucidated. We previously reported that acetaminophen (APAP) induces CYP3A activity via inhibition of protein degradation and proposed a novel DDI concept. N-Acetyl-p-benzoquinone imine (NAPQI), the reactive metabolite of APAP formed by CYP, is known to cause adverse events related to depletion of intracellular reduced glutathione (GSH)...
March 21, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28340593/erratum-to-aryl-hydrocarbon-receptor-cytochrome-p450-1a1-pathway-mediates-breast-cancer-stem-cells-expansion-through-pten-inhibition-and-%C3%AE-catenin-and-akt-activation
#15
Abdullah Al-Dhfyan, Ali Alhoshani, Hesham M Korashy
No abstract text is available yet for this article.
March 24, 2017: Molecular Cancer
https://www.readbyqxmd.com/read/28340555/rna-seq-transcriptomics-and-pathway-analyses-reveal-potential-regulatory-genes-and-molecular-mechanisms-in-high-and-low-residual-feed-intake-in-nordic-dairy-cattle
#16
M S Salleh, G Mazzoni, J K Höglund, D W Olijhoek, P Lund, P Løvendahl, H N Kadarmideen
BACKGROUND: The selective breeding of cattle with high-feed efficiencies (FE) is an important goal of beef and dairy cattle producers. Global gene expression patterns in relevant tissues can be used to study the functions of genes that are potentially involved in regulating FE. In the present study, high-throughput RNA sequencing data of liver biopsies from 19 dairy cows were used to identify differentially expressed genes (DEGs) between high- and low-FE groups of cows (based on Residual Feed Intake or RFI)...
March 24, 2017: BMC Genomics
https://www.readbyqxmd.com/read/28340451/the-role-of-drug-drug-interactions-in-prostate-cancer-treatment-focus-on-abiraterone-acetate-prednisone-and-enzalutamide
#17
REVIEW
Marzia Del Re, Stefano Fogli, Lisa Derosa, Francesco Massari, Paul De Souza, Stefania Crucitta, Sergio Bracarda, Daniele Santini, Romano Danesi
Elderly patients with cancer may have comorbidities, each requiring additional pharmacologic treatment. Therefore, the occurrence of pharmacokinetic (PK) and pharmacodynamic (PD) interactions is very likely, and the risk of adverse reactions (ADRs), due to the narrow therapeutic window of anticancer drugs, is increased. Drug-drug interactions (DDIs) may occur in prostate cancer patients due to inhibition by abiraterone of liver cytochrome P450 (CYP)-dependent enzymes CYP2C8 and 2D6, which are involved in the metabolism of approximately 25% of all drugs, and induction by enzalutamide of CYP3A4, 2C9 and 2C19, which metabolize up to 50% of medications...
March 9, 2017: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/28339191/allosteric-activation-of-cytochrome-p450-3a4-via-progesterone-bioconjugation
#18
Vanja Polic, Karine Auclair
Human cytochrome P450 3A4 (CYP3A4) is responsible for the metabolism of the majority of drugs. As such, it is implicated in many adverse drug-drug and food-drug interactions, and is of significant interest to the pharmaceutical industry. This enzyme is known to simultaneously bind multiple ligands and display atypical enzyme kinetics, suggestive of allostery and cooperativity. As well, evidence of a postulated peripheral allosteric binding site has provoked debate around its significance and location. We report the use of bioconjugation to study the significance of substrate binding at the proposed allosteric site and its effect on CYP3A4 activity...
March 24, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28339022/cytochrome-p450-2e1-increases-the-sensitivity-of-hepatoma-cells-to-vitamin-k2
#19
Lu Li, Lu Wang, Rui Song, Guangliang Chen, Yanyan Liu
Although vitamin K2 (VK2) exhibits inhibitory effects on the viability of hepatoma cells, hepatoma cells are insensitive to VK2. Therefore, this investigation is an attempt to enhance the sensitivity of hepatoma cells to VK2. Our results showed that VK2 acted synergistically with ethanol (EtOH) to inhibit the viability of Smmc-7721 cells, mainly because cytochrome P450 2E1 (CYP2E1) was activated by EtOH. The synergistic effect of VK2 and EtOH was also observed in QGY-7703 cells, which also express CYP2E1. However, in HepG2 cells, which do not express CYP2E1, the synergistic effect of VK2 and EtOH was not observed...
March 24, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28338801/evolutionary-origin-of-mitochondrial-cytochrome-p450
#20
Tsuneo Omura, Osamu Gotoh
Different molecular species of cytochrome P450 (P450) are distributed between endoplasmic reticulum (microsomes) and mitochondria in animal cells. Plants and fungi have many microsomal P450s, but no mitochondrial P450 has so far been reported. To elucidate the evolutionary origin of mitochondrial P450s in animal cells, available evidence is examined, and the virtual absence of mitochondrial P450 in plants and fungi is confirmed. It is also suggested that a microsomal P450 is the ancestor of animal mitochondrial P450s...
March 7, 2017: Journal of Biochemistry
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