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cytochrom p450

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https://www.readbyqxmd.com/read/29031061/crassiflorone-derivatives-that-inhibit-trypanosoma-brucei-glyceraldehyde-3-phosphate-dehydrogenase-tbgapdh-and-trypanosoma-cruzi-trypanothione-reductase-tctr-and-display-trypanocidal-activity
#1
Elisa Uliassi, Giulia Fiorani, R Luise Krauth-Siegel, Christian Bergamini, Romana Fato, Giulia Bianchini, J Carlos Menéndez, Maria Teresa Molina, Eulogio López-Montero, Federico Falchi, Andrea Cavalli, Sheraz Gul, Maria Kuzikov, Bernhard Ellinger, Gesa Witt, Carolina B Moraes, Lucio H Freitas-Junior, Chiara Borsari, Maria Paola Costi, Maria Laura Bolognesi
Crassiflorone is a natural product with anti-mycobacterial and anti-gonorrhoeal properties, isolated from the stem bark of the African ebony tree Diospyros crassiflora. We noticed that its pentacyclic core possesses structural resemblance to the quinone-coumarin hybrid 3, which we reported to exhibit a dual-targeted inhibitory profile towards Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH) and Trypanosoma cruzi trypanothione reductase (TcTR). Following this basic idea, we synthesized a small library of crassiflorone derivatives 15-23 and investigated their potential as anti-trypanosomatid agents...
October 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29029351/development-and-application-of-a-dual-rat-and-human-ahr-activation-assay
#2
Martin R Brown, Helen Garside, Emma Thompson, Saseela Atwal, Chloe Bean, Tony Goodall, Michael Sullivan, Mark J Graham
Significant prolonged AHR activation, classically exhibited following exposure to TCDD (dioxin), can cause a variety of undesirable toxicological effects. Novel pharmaceutical chemistries also have the potential to cause activation of AHR and consequent toxicities in pre-clinical species and man. Previous methods either employed relatively expensive and low throughput primary hepatocyte dosing with PCR endpoint, or low resolution overexpressing reporter gene assays. We have developed, validated and applied an in vitro microtitre plate imaging-based medium throughput screening assay for the assessment of endogenous species-specific AHR activation potential via detection of induction of the surrogate transcriptional target Cytochrome P450 CYP1A1...
September 18, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29029135/small-increase-in-dolutegravir-trough-but-equivalent-total-dolutegravir-exposure-with-simeprevir-in-hiv-hcv-seronegative-volunteers
#3
Christine E MacBrayne, Jose Castillo-Mancilla, James R Burton, Samantha MaWhinney, Charlotte B Wagner, Kestutis Micke, Jordan Fey, Ryan T Huntley, Bayli Larson, Lane R Bushman, Jennifer J Kiser
Background: Dolutegravir, an HIV integrase strand-transfer inhibitor, and simeprevir, an HCV NS3/4A PI, have the potential to interact as dolutegravir is a P-glycoprotein, uridine glucuronosyl transferase 1A1 and cytochrome P450 3A substrate and simeprevir has been shown to mildly inhibit these. Objectives: To compare dolutegravir and simeprevir pharmacokinetics (PK) when given separately versus in combination. Methods: Healthy volunteers received: (i) 150 mg of simeprevir once daily for 7 days; (ii) 50 mg of dolutegravir once daily for 7 days; and (iii) 150 mg of simeprevir once daily plus 50 mg of dolutegravir once daily for 7 days, with randomization to treatment sequence...
October 4, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29027939/nicotine-component-of-cigarette-smoke-extract-cse-decreases-the-cytotoxicity-of-cse-in-beas-2b-cells-stably-expressing-human-cytochrome-p450-2a13
#4
Minghui Ji, Yudong Zhang, Na Li, Chao Wang, Rong Xia, Zhan Zhang, Shou-Lin Wang
Cytochrome P450 2A13 (CYP2A13), an extrahepatic enzyme mainly expressed in the human respiratory system, has been reported to mediate the metabolism and toxicity of cigarette smoke. We previously found that nicotine inhibited 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) metabolism by CYP2A13, but its influence on other components of cigarette smoke remains unclear. The nicotine component of cigarette smoke extract (CSE) was separated, purified, and identified using high-performance liquid chromatography (HPLC) and ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS), splitting CSE into a nicotine section (CSE-N) and nicotine-free section (CSE-O)...
October 13, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/29027484/cyp1a1-expression-and-organochlorine-pesticides-level-in-the-etiology-of-bladder-cancer-in-north-indian-population
#5
H Verma, T Sharma, S Gupta, B D Banerjee
Urinary bladder cancer (UBC) is one of the most common malignancies worldwide. The etiology of UBC is multifactorial and includes both exogenous and endogenous factors. Exogenous risk factors include exposure to heavy metals, aromatic amines, and environmental pollutants including pesticides such as organochlorine pesticides (OCPs). Environmental factors alone are incapable of directly producing DNA damage and may require activation by phase I metabolizing enzymes like cytochrome P450 in order to become active carcinogen...
January 1, 2017: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/29027214/development-of-an-alternative-zebrafish-model-for-drug-induced-intestinal-toxicity
#6
Bokyeong Ryu, C-Yoon Kim, Hanseul Oh, Ukjin Kim, Jin Kim, Cho-Rok Jung, Byoung-Hee Lee, Seungki Lee, Seo-Na Chang, Ji Min Lee, Hyung-Min Chung, Jae-Hak Park
An evaluation of intestinal toxicity is important because the mucosal lining of the gastrointestinal tract is the first barrier for oral xenobiotics. Until now, a rat model has been recommended as the standard intestinal toxicity model and the Caco-2 cell line, originated from a human colon adenocarcinoma, has been used as an alternative to this model, but there are limitations regarding cost-effectiveness and the need for mimicry of the human system. In this study, we investigated whether zebrafish could be a valid alternative to rats and Caco-2 cells as an intestinal toxicity model...
October 13, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/29027195/tspyl-family-regulates-cyp17a1-and-cyp3a4-expression-potential-mechanism-contributing-to-abiraterone-response-in-metastatic-castration-resistant-prostate-cancer
#7
Sisi Qin, Duan Liu, Manish Kohli, Liguo Wang, Peter T Vedell, David W Hillman, Nifang Niu, Jia Yu, Richard M Weinshilboum, Liewei Wang
The testis-specific Y-encoded-like protein (TSPYL) gene family includes TSPYL1 to TSPYL6. We previously reported that TSPYL5 regulates cytochrome P450 (CYP) 19A1 expression. Here, we show that TSPYLs, especially, TSPYL 1, 2 and 4, can regulate the expression of many CYP genes, including CYP17A1, a key enzyme in androgen biosynthesis, and CYP3A4, an enzyme that catalyzes the metabolism of abiraterone, a CYP17 inhibitor. Furthermore, a common TSPYL1 SNP, rs3828743 (G/A) (Pro62Ser), abolishes TSPYL1's ability to suppress CYP3A4 expression, resulting in reduced abiraterone concentrations and increased cell proliferation...
October 13, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29026425/effect-of-cytochrome-p450-2c19-17-allelic-variant-on-cardiovascular-and-cerebrovascular-outcomes-in-clopidogrel-treated-patients-a-systematic-review-and-meta-analysis
#8
REVIEW
Bo Huang, De-Jun Cui, Ying Ren, Bin Han, Da-Ping Yang, Xun Zhao
BACKGROUND: We aimed to evaluate the associations of gain-of-function allele of CYP2C19*17 and risk of clinical events in clopidogrel-treated patients with cardiovascular and cerebrovascular diseases (CCVDs). MATERIALS AND METHODS: Literature search was conducted in PubMed, EMBASE, and Cochrane Library. Odds ratio (OR) combined with 95% confidence interval (CI) was the pooled statistics. Subgroup analysis was performed by disease type, bleeding events, and race...
2017: Journal of Research in Medical Sciences: the Official Journal of Isfahan University of Medical Sciences
https://www.readbyqxmd.com/read/29026041/anti-markovnikov-alkene-oxidation-by-metal-oxo-mediated-enzyme-catalysis
#9
Stephan C Hammer, Grzegorz Kubik, Ella Watkins, Shan Huang, Hannah Minges, Frances H Arnold
Catalytic anti-Markovnikov oxidation of alkene feedstocks could simplify synthetic routes to many important molecules and solve a long-standing challenge in chemistry. Here we report the engineering of a cytochrome P450 enzyme by directed evolution to catalyze metal-oxo-mediated anti-Markovnikov oxidation of styrenes with high efficiency. The enzyme uses dioxygen as the terminal oxidant and achieves selectivity for anti-Markovnikov oxidation over the kinetically favored alkene epoxidation by trapping high-energy intermediates and catalyzing an oxo transfer, including an enantioselective 1,2-hydride migration...
October 13, 2017: Science
https://www.readbyqxmd.com/read/29025271/psychotropic-drugs-and-cyp2d6-in-late-life-psychiatric-and-neurological-disorders-what-do-we-know
#10
Davide Seripa, Madia Lozupone, Eleonora Stella, Giulia Paroni, Paola Bisceglia, Maddalena La Montagna, Grazia D'onofrio, Carolina Gravina, Maria Urbano, Maria Giovanna Priore, Angela Lamanna, Antonio Daniele, Antonello Bellomo, Giancarlo Logroscino, Antonio Greco, Francesco Panza
Late-life psychiatric and neurological disorders (LLPND) are interesting models to understand the potential role of pharmacogenetics in drug management, since several pharmacological approaches for treating LLPND have proven to be ineffective or deleterious, thus resulting in therapeutic failures (TF) and adverse drug reactions (ADR). Common variants in the genes encoding the cytochrome P450 (CYP) enzyme system, the 'engine room' of drug metabolism, together with well-known age-related increased polypharmacy also contributed to the prevalence of TF and ADR observed in these patients, also rising number and time of hospital readmissions and rate of institutionalizations...
October 12, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/29024742/cyp-mediated-drug-metabolism-in-the-brain-impacts-drug-response
#11
REVIEW
Douglas M McMillan, Rachel F Tyndale
The functional role of cytochrome P450 (CYP) enzymes in the brain is an exciting and evolving field of research. CYPs are present and active in the brain, with heterogeneous patterns of expression, activity, and sensitivity to modulation across cell types, regions, and species. Despite total brain CYP expression being a fraction of hepatic CYP expression, the expanding literature of in vitro and in vivo experiments have provided evidence that brain CYPs can impact acute and chronic drug response, susceptibility to damage by neurotoxins, and are associated with altered personality, behaviour, and risk of neurological disease...
October 9, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29024717/supplementation-of-american-ginseng-berry-extract-mitigated-cisplatin-evoked-nephrotoxicity-by-suppressing-ros-mediated-activation-of-mapk-and-nf-%C3%AE%C2%BAb-signaling-pathways
#12
Zhi-Na Ma, Zhi Liu, Zi Wang, Shen Ren, Shan Tang, Ying-Ping Wang, Sheng-Yuan Xiao, Chen Chen, Wei Li
Nephrotoxicity induced by cisplatin in 30% of all cisplatin treated patients seriously limits its clinical implication as a widely used anticancer agent, and may even cause patients to alter or give up cisplatin therapy. The purpose of this study is to test a protective effect of American ginseng berry extract (AGBE) on cisplatin-induced nephrotoxicity in mice. In this study, the histopathological changes and elevated levels of serum creatinine (CRE) and urea nitrogen (BUN) caused by cisplatin were significantly diminished by AGBE treatment...
October 9, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29024391/orthogonal-expression-of-an-artificial-metalloenzyme-for-abiotic-catalysis
#13
Eric Brustad, Evan W Reynolds, Timothy D Schwochert, Matthew W McHenry, John W Watters
A cytochrome P450 was engineered to selectively incorporate Ir(Me)-deuteroporphyrin IX (Ir(Me)-DPIX), in lieu of heme, in bacterial cells. Cofactor selectivity was altered by introducing mutations within the heme-binding pocket that discriminate the deuteroporphyrin macrocycle, in combination with mutations to the P450 axial cysteine to accommodate a pendant methyl group on the Ir(Me)-center. This artificial metalloenzyme was investigated for activity in non-native metallocarbenoid-mediated olefin cyclopropanation reactions and showed enhanced activity for aliphatic and electron-deficient olefins when compared to the native heme enzyme...
October 11, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/29023376/altered-protein-expression-of-cardiac-cyp2j-and-hepatic-cyp2c-cyp4a-and-cyp4f-in-a-mouse-model-of-type-ii-diabetes-a-link-in-the-onset-and-development-of-cardiovascular-disease
#14
Benoit Drolet, Sylvie Pilote, Carolanne Gélinas, Alida-Douce Kamaliza, Audrey Blais-Boilard, Jessica Virgili, Dany Patoine, Chantale Simard
Arachidonic acid can be metabolized by cytochrome P450 (CYP450) enzymes in a tissue- and cell-specific manner to generate vasoactive products such as epoxyeicosatrienoic acids (EETs-cardioprotective) and hydroxyeicosatetraenoic acids (HETEs-cardiotoxic). Type II diabetes is a well-recognized risk factor for developing cardiovascular disease. A mouse model of Type II diabetes (C57BLKS/J-db/db) was used. After sacrifice, livers and hearts were collected, washed, and snap frozen. Total proteins were extracted...
October 12, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29023357/pharmacokinetics-safety-and-efficacy-of-maraviroc-in-treatment-experienced-pediatric-patients-infected-with-ccr5-tropic-hiv-1
#15
Carlo Giaquinto, Muthuhadini Patience Mawela, Kulkanya Chokephaibulkit, Marinella Della Negra, Ismail Haroon Mitha, Jan Fourie, Annie Fang, Elna van der Ryst, Srinivas Rao Valluri, Manoli Vourvahis, Rebecca Yanhui Zhang-Roper, Charles Craig, Lynn McFadyen, Andrew Clark, Jayvant Heera
BACKGROUND: Maraviroc is a CCR5 antagonist approved to treat adults infected with CCR5-tropic (R5) HIV-1. Study A4001031 was conducted to evaluate the pharmacokinetics, safety, and efficacy of maraviroc in combination with optimized background therapy (OBT) in treatment-experienced pediatric patients infected with R5 HIV-1 and support registration of maraviroc for pediatric use. METHODS: This is an open-label, 2-stage, age-stratified, non-comparative multicenter study...
October 7, 2017: Pediatric Infectious Disease Journal
https://www.readbyqxmd.com/read/29023140/genetic-polymorphisms-of-cytochrome-p450-enzymes-and-transport-proteins-in-a-russian-population-and-three-ethnic-groups-of-dagestan
#16
Karin B Mirzaev, Dmitry A Sychev, Kristina A Ryzhikova, Olga D Konova, Suleiman N Mammaev, Daniyal M Gafurov, Grigorij N Shuev, Elena A Grishina, Zhannet A Sozaeva
AIM: The objective of this study was to investigate the prevalence of polymorphic markers of the CYP2C19, CYP2C9, CYP2D6, SLCO1B1, and ABCB1 genes among the three ethnic groups in Dagestan and compare it with the carrier frequency of these markers among the Russian population living in Moscow. METHODS: The study involved 186 healthy, unrelated, and chronic medication-free volunteers (53 males and 133 females) of the three ethnic groups in the Dagestan Republic: 46 Laks, 90 Avars, and 50 Dargins...
October 12, 2017: Genetic Testing and Molecular Biomarkers
https://www.readbyqxmd.com/read/29022838/pharmacogenomics-of-triazole-antifungal-agents-implications-for-safety-tolerability-and-efficacy
#17
Jarrett R Amsden, Paul O Gubbins
Introduction Triazole antifungal agents are prescribed to treat invasive fungal infections in neutropenic and non-neutropenic patients. These antifungal agents are substrates and inhibitors of cytochrome P450 (CYP). Genetic polymorphisms in CYP2C9, CYP2C19 and CYP3A5 can lead to large population-specific variations in drug efficacy and safety, optimal dosing, or contribute to drug interactions associated with this class. Areas covered This manuscript reviews the pharmacogenomics (i.e. the influence of genetics on drug disposition) of triazole antifungal agents related to their CYP-mediated metabolism and summarizes their implications on triazole efficacy, safety, and tolerability...
October 12, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29022765/polymorphisms-in-genes-involved-in-vasoactive-eicosanoids-synthesis-affect-cardiovascular-risk-in-renal-transplant-recipients
#18
Guillermo Gervasini, Enrique Luna, Guadalupe Garcia-Pino, Lilia Azevedo, Sonia Mota-Zamorano, Juan José Cubero
OBJECTIVE: Arachidonic acid metabolism by cytochrome P450 (CYP) epoxygenases lead to epoxyeicosatrienoic acids (EETs), which eicosanoids with vasodilator and anti-inflammatory properties. We aim to determine whether genetic variability in these routes may contribute to cardiovascular (CV) risk in renal transplant recipients. METHODS: In a cohort of 355 patients, we determined the presence of two polymorphisms, CYP2C8*3 and CYP2J2*7, known to affect eicosanoids levels...
October 12, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/29022574/osthole-prevents-acetaminophen-induced-liver-injury-in-mice
#19
Yun Cai, Wu Sun, Xin-Xin Zhang, Yan-Die Lin, Hao Chen, Hao Li
Acetaminophen (APAP) overdose leads to severe hepatotoxicity. Osthole, a natural coumarin found in traditional Chinese medicinal herbs, has therapeutic potential in the treatment of various diseases. In this study, we investigated the effects of osthole against APAP-induced hepatotoxicity in mice. Mice were administered osthole (100 mg·kg(-1)·d(-1), ip) for 3 d, then on the fourth day APAP (300 mg/kg, ip) was co-administered with osthole. The mice were euthanized post-APAP, their serum and livers were collected for analysis...
October 12, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29022184/effects-of-ketoconazole-on-the-pharmacokinetics-of-mifepristone-a-competitive-glucocorticoid-receptor-antagonist-in-healthy-men
#20
Dat Nguyen, Sarah Mizne
INTRODUCTION: Mifepristone, a competitive glucocorticoid receptor antagonist approved for Cushing syndrome, and ketoconazole, an antifungal and steroidogenesis inhibitor, are both inhibitors of and substrates for cytochrome P450 (CYP3A4). This study evaluated the pharmacokinetic effects of concomitant ketoconazole, a strong CYP3A4 inhibitor, on mifepristone. METHODS: In an open-label, two-period, single-center study, healthy adult men received mifepristone 600 mg orally daily for 12 days (period 1) followed by mifepristone 600 mg daily plus ketoconazole 200 mg orally twice daily for 5 days (period 2)...
October 11, 2017: Advances in Therapy
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