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https://www.readbyqxmd.com/read/29329342/ternary-copper-ii-complex-nci60-screening-toxicity-studies-and-evaluation-of-efficacy-in-xenograft-models-of-nasopharyngeal-carcinoma
#1
Munirah Ahmad, Shazlan-Noor Suhaimi, Tai-Lin Chu, Norazlin Abdul Aziz, Noor-Kaslina Mohd Kornain, D S Samiulla, Kwok-Wai Lo, Chew-Hee Ng, Alan Soo-Beng Khoo
Copper(II) ternary complex, [Cu(phen)(C-dmg)(H2O)]NO3 was evaluated against a panel of cell lines, tested for in vivo efficacy in nasopharyngeal carcinoma xenograft models as well as for toxicity in NOD scid gamma mice. The Cu(II) complex displayed broad spectrum cytotoxicity against multiple cancer types, including lung, colon, central nervous system, melanoma, ovarian, and prostate cancer cell lines in the NCI-60 panel. The Cu(II) complex did not cause significant induction of cytochrome P450 (CYP) 3A and 1A enzymes but moderately inhibited CYP isoforms 1A2, 2C9, 2C19, 2D6, 2B6, 2C8 and 3A4...
2018: PloS One
https://www.readbyqxmd.com/read/29326811/impact-of-liver-volume-and-liver-function-on-posthepatectomy-liver-failure-after-portal-vein-embolization-a-multivariable-cohort-analysis
#2
Patrick H Alizai, Annabel Haelsig, Philipp Bruners, Florian Ulmer, Christian D Klink, Cornelis H C Dejong, Ulf P Neumann, Maximilian Schmeding
Background: Liver failure remains a life-threatening complication after liver resection, and is difficult to predict preoperatively. This retrospective cohort study evaluated different preoperative factors in regard to their impact on posthepatectomy liver failure (PHLF) after extended liver resection and previous portal vein embolization (PVE). Methods: Patient characteristics, liver function and liver volumes of patients undergoing PVE and subsequent liver resection were analyzed...
January 2018: Annals of Medicine and Surgery
https://www.readbyqxmd.com/read/29318639/interaction-between-caffeine-and-polymorphisms-of-glutamate-ionotropic-receptor-nmda-type-subunit-2a-grin2a-and-cytochrome-p450-1a2-cyp1a2-on-parkinson-s-disease-risk
#3
Iris Y Kim, Éilis J O'Reilly, Katherine C Hughes, Xiang Gao, Michael A Schwarzschild, Marjorie L McCullough, Marian T Hannan, Rebecca A Betensky, Alberto Ascherio
BACKGROUND: Caffeine intake has been inversely associated with Parkinson's disease (PD) risk. This relationship may be modified by polymorphisms of glutamate ionotropic receptor NMDA type subunit 2A (GRIN2A) and cytochrome P450 1A2 (CYP1A2), but the results of previous studies have been inconsistent. METHOD: We examined the interaction of caffeine intake with GRIN2A-rs4998386 and CYP1A2-rs762551 polymorphisms in influencing PD risk among 829 incident cases of PD and 2,754 matched controls selected among participants in the following 3 large prospective ongoing cohorts: the Nurses' Health Study, the Health Professionals' Follow-up Study, and the Cancer Prevention Study II Nutrition Cohort...
January 10, 2018: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/29310511/cytochrome-p450-2a6-and-other-human-p450-enzymes-in-the-oxidation-of-flavone-and-flavanone
#4
Kensaku Kakimoto, Norie Murayama, Shigeo Takenaka, Haruna Nagayoshi, Young-Ran Lim, Vitchan Kim, Donghak Kim, Hiroshi Yamazaki, Masayuki Komori, F Peter Guengerich, Tsutomu Shimada
1. We previously reported that flavone and flavanone interact spectrally with cytochrome P450 (P450 or CYP) 2A6 and 2A13 and other human P450s and inhibit catalytic activities of these P450 enzymes. In this study, we studied abilities of CYP1A1, 1A2, 1B1, 2A6, 2A13, 2C9, and 3A4 to oxidize flavone and flavanone. 2. Human P450s oxidized flavone to 6- and 5-hydroxylated flavones, seven uncharacterized mono-hydroxylated flavones, and five di-hydroxylated flavones. CYP2A6 was most active in forming 6-hydroxy- and 5-hydroxyflavones and several mono- and di-hydroxylated products...
January 9, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29306656/association-between-a-microrna-binding-site-polymorphism-in-slco1a2-and-the-risk-of-delayed-methotrexate-elimination-in-chinese-children-with-acute-lymphoblastic-leukemia
#5
Shu-Mei Wang, Wei-Xin Zeng, Wan-Shui Wu, Lu-Lu Sun, Dan Yan
Organic anion-transporting polypeptide 1A2 (OATP1A2) is involved in the cellular uptake of methotrexate (MTX). Genetic variation in solute carrier organic anion transporter family member 1A2 (SLCO1A2, the coding gene of OATP1A2) has important implications for the elimination of MTX. We investigated the association between a microRNA (miRNA) binding site polymorphism (rs4149009 G > A) in the 3'-untranslated region (3'-UTR) of SLCO1A2 with the serum MTX concentrations in Chinese children with acute lymphoblastic leukemia (ALL)...
January 2, 2018: Leukemia Research
https://www.readbyqxmd.com/read/29285606/the-formation-of-estrogen-like-tamoxifen-metabolites-and-their-influence-on-enzyme-activity-and-gene-expression-of-adme-genes
#6
Janina Johänning, Patrick Kröner, Maria Thomas, Ulrich M Zanger, Astrid Nörenberg, Michel Eichelbaum, Matthias Schwab, Hiltrud Brauch, Werner Schroth, Thomas E Mürdter
Tamoxifen, a standard therapy for breast cancer, is metabolized to compounds with anti-estrogenic as well as estrogen-like action at the estrogen receptor. Little is known about the formation of estrogen-like metabolites and their biological impact. Thus, we characterized the estrogen-like metabolites tamoxifen bisphenol and metabolite E for their metabolic pathway and their influence on cytochrome P450 activity and ADME gene expression. The formation of tamoxifen bisphenol and metabolite E was studied in human liver microsomes and Supersomes™...
December 28, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29282363/the-impact-of-genetic-polymorphisms-on-cyp1a2-activity-in-humans-a-systematic-review-and-meta-analysis
#7
Nut Koonrungsesomboon, Rapheephorn Khatsri, Penwisa Wongchompoo, Supanimit Teekachunhatean
A large interindividual variation in the activity of cytochrome P450 1A2 (CYP1A2) raises concern about therapeutic failure or toxicity when medical professionals prescribe drugs extensively metabolized by CYP1A2. To date, a number of studies have assessed the association between genetic polymorphisms and CYP1A2 activity; however, there are controversies as to the functional importance of CYP1A2 polymorphisms on the metabolism of CYP1A2 substrates. This systematic review and meta-analysis assessed the effects of genetic polymorphisms on CYP1A2 activity, as measured by caffeine metabolism, in a total of 3570 individual subjects...
December 27, 2017: Pharmacogenomics Journal
https://www.readbyqxmd.com/read/29242757/differential-gene-transcription-of-extracellular-matrix-components-in-response-to-in-vivo-corneal-crosslinking-cxl-in-rabbit-corneas
#8
Sabine Kling, Arthur Hammer, Emilio A Torres Netto, Farhad Hafezi
Purpose: We studied changes in gene transcription after corneal crosslinking (CXL) in the rabbit cornea in vivo and identified potential molecular signaling pathways. Methods: A total of 15 corneas of eight male New-Zealand-White rabbits were de-epithelialized and equally divided into five groups. Group 1 served as an untreated control. Groups 2 to 5 were soaked with 0.1% riboflavin for 20 minutes, which in Groups 3 to 5 was followed by UV-A irradiation at a fluence of 5...
December 2017: Translational Vision Science & Technology
https://www.readbyqxmd.com/read/29237928/correlations-between-mitofusin-2-expression-in-fibroblasts-and-pelvic-organ-prolapse-an-in-vitro-study
#9
Ye Lu, Hua-Yun Chen, Xiao-Qing Wang, Jing-Xue Wang
BACKGROUND: Both Mitofusin 2 (Mfn2) and pelvic organ prolapse (POP) are related to aging. The aim of the present study was to investigate the variations of Mfn2 expression in the uterosacral ligaments of patients with and/or without POP and their correlations with the expression of procollagen. METHODS: Fibroblasts were cultured using tissue specimens that were harvested from the uterosacral ligaments of POP and non-POP (NPOP) patients (n = 10 for each group) from September 2016 to December 2016...
December 20, 2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/29219051/development-and-uses-of-offline-and-web-searchable-metabolism-databases-the-case-of-benzo-a-pyrene
#10
Slobodan P Rendic, F Peter Guengerich
The paper presents development and use of offline and Web-searchable human and other species metabolism databases. A search of the databases presented will produce basic information on metabolic reactions or transporter systems published on specific drug or other chemical, kinetic values, as well as structure of the metabolites. In addition, searching enables comparison of the data between different species models. The data cover time the period until 2008, and the current Web-searchable database [19] is updated quarterly each year and over the period until October 2017...
December 7, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/29211304/risk-of-recurrence-prognosis-and-follow-up-for-danish-women-with-cervical-cancer-in-2005-2013-a-national-cohort-study
#11
Gry Assam Taarnhøj, Ib Jarle Christensen, Henrik Lajer, Katrine Fuglsang, Mette Moustgaard Jeppesen, Henriette Strøm Kahr, Claus Høgdall
BACKGROUND: In developed countries, women attend follow-up after treatment for cervical cancer to detect recurrence. The aim of this study was to describe the Danish population of women with early-stage cervical cancer at risk for recurrence and death due to recurrence. METHODS: Data were extracted from 3 nationwide databases to find women diagnosed with stage 1A1 to 1B1 cervical cancer in 2005-2013. Recurrences were determined from data on oncological or surgical treatment more than 3 months after the initial diagnosis and were cross-checked with patient journals...
December 6, 2017: Cancer
https://www.readbyqxmd.com/read/29202402/design-synthesis-and-biological-evaluation-of-a-series-of-resorcinol-based-n-benzyl-benzamide-derivatives-as-potent-hsp90-inhibitors
#12
Sun You Park, Yong Jin Oh, Yunmee Lho, Ju Hui Jeong, Kwang-Hyeon Liu, Jaeyoung Song, Soong-Hyun Kim, Eunyoung Ha, Young Ho Seo
Heat shock protein 90 (Hsp90) is a ubiquitous molecular chaperone that is responsible for the stabilization and maturation of many oncogenic proteins. Therefore, Hsp90 has emerged as an attractive target in the field of cancer chemotherapy. In this study, we report the design, synthesis, and biological evaluation of a series of Hsp90 inhibitors. In particular, compound 30f shows a significant Hsp90α inhibitory activity with IC50 value of 5.3 nM and an excellent growth inhibition with GI50 value of 0.42 μM against non-small cell lung cancer cells, H1975...
November 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29197979/genetic-differences-in-the-aryl-hydrocarbon-receptor-and-cyp1a2-affect-sensitivity-to-developmental-polychlorinated-biphenyl-exposure-in-mice-relevance-to-studies-of-human-neurological-disorders
#13
Kelsey Klinefelter, Molly Kromme Hooven, Chloe Bates, Breann T Colter, Alexandra Dailey, Smitha Krishnan Infante, Izabela Kania-Korwel, Hans-Joachim Lehmler, Alejandro López-Juárez, Clare Pickering Ludwig, Christine Perdan Curran
Polychlorinated biphenyls (PCBs) are persistent organic pollutants that remain a human health concern with newly discovered sources of contamination and ongoing bioaccumulation and biomagnification. Children exposed during early brain development are at highest risk of neurological deficits, but highly exposed adults reportedly have an increased risk of Parkinson's disease. Our previous studies found allelic differences in the aryl hydrocarbon receptor and cytochrome P450 1A2 (CYP1A2) affect sensitivity to developmental PCB exposure, resulting in cognitive deficits and motor dysfunction...
December 2, 2017: Mammalian Genome: Official Journal of the International Mammalian Genome Society
https://www.readbyqxmd.com/read/29176019/in-vitro-modulation-of-the-cytochrome-p450-and-abcb1-p-glycoprotein-activities-of-the-aqueous-extract-of-allophylus-cominia-l-sw-leaves
#14
Carlos L Pérez, Maria T Donato, Ivones Hernández, Miriam T Paz Lopes, Evangelina Marrero, Jose A Herrera, Maria J Gómez-Lechón, Idania Rodeiro
BACKGROUND: The aqueous extract of the Allophylus cominia (L) Sw (Sapindaceae) leaves has shown anti-diabetic, anti-obesity and anti-inflammatory properties. In the Caribbean region, it is typically used for the treatment of type-2 diabetes. METHODS: Considering the herb-drug interaction, the aim of this study was to evaluate the potential effects of the A. cominia extract on the cytochrome P450 (CYP) (rat hepatocyte model) and P-glycoprotein (P-gp) (4T1 cell line) systems...
November 25, 2017: Drug Metabolism and Personalized Therapy
https://www.readbyqxmd.com/read/29155491/variation-in-the-response-of-clozapine-biotransformation-pathways-in-human-hepatic-microsomes-to-cyp1a2-and-cyp3a4-selective-inhibitors
#15
Michael Murray, Wei V Zhang, Robert J Edwards
The atypical antipsychotic agent clozapine (CLZ) is effective in many patients who are resistant to conventional antipsychotic drugs. Cytochromes P450 (CYPs) 1A2 and 3A4 oxidise CLZ to norCLZ and CLZ N-oxide in human liver. Concurrent treatment with inducers and inhibitors of CYP1A2 modulates CLZ elimination that disrupts therapy. Drug-drug interactions involving CYP3A4 are also significant but less predictable. To further characterise the factors underlying these interactions, we used samples from a cohort of human livers to assess variation in CLZ oxidation pathways in relation to intrinsic CYP3A4 and CYP1A2 activities and the effects of the corresponding selective inhibitors ketoconazole (0...
November 20, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29143794/berberine-activates-aryl-hydrocarbon-receptor-but-suppresses-cyp1a1-induction-through-mir-21-3p-stimulation-in-mcf-7-breast-cancer-cells
#16
Sheng-Nan Lo, Chun-Wei Wang, Yueh-Shieh Chen, Chiung-Chiao Huang, Tian-Shung Wu, Lih-Ann Li, I-Jung Lee, Yune-Fang Ueng
Berberine and the methylenedioxy ring-opening derivatives palmatine and jatrorrhizine are active ingredients in immunomodulatory plants, such as goldenseal. This study aimed to illustrate the effects of protoberberines on aryl hydrocarbon receptor (AhR) activation and cytochrome P450 (CYP) 1 in the estrogen receptor (ER)α(+) MCF-7 breast cancer cells. Among protoberberines at non-cytotoxic concentrations (≤10 μM), berberine had the most potent and statistically significant effects on AhR activation and CYP1A1/1A2/1B1 mRNA induction...
October 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29138024/-e-3-3-4-5-trimethoxyphenyl-1-pyridin-4-yl-prop-2-en-1-one-a-heterocyclic-chalcone-is-a-potent-and-selective-cyp1a1-inhibitor-and-cancer-chemopreventive-agent
#17
Neill J Horley, Kenneth J M Beresford, Supriya Kaduskar, Prashant Joshi, Glen J P McCann, Ketan C Ruparelia, Ibidapo S Williams, Linda Gatchie, Vinay R Sonawane, Sandip B Bharate, Bhabatosh Chaudhuri
The overexpression of CYP1 family of enzymes is reported to be associated with development of human carcinomas. It has been well reported that CYP1A1 specific inhibitors prevents carcinogenesis. Herein, thirteen pyridine-4-yl series of chalcones were synthesized and screened for inhibition of CYP1 isoforms 1A1, 1B1 and 1A2 in Sacchrosomes™ and live human HEK293 cells. The structure-activity relationship analysis indicated that chalcones bearing tri-alkoxy groups (8a and 8k) on non-heterocyclic ring displayed selective inhibition of CYP1A1 enzyme, with IC50 values of 58 and 65 nM, respectively...
November 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29136681/assessment-of-multiple-cytochrome-p450-activities-in-metabolically-inactivated-human-liver-microsomes-and-roles-of-p450-2c-isoforms-in-reaction-phenotyping-studies
#18
Norie Murayama, Kanako Yajima, Mikiko Hikawa, Kanami Shimura, Yu Ishii, Masaki Takada, Yasuhiro Uno, Masahiro Utoh, Kazuhide Iwasaki, Hiroshi Yamazaki
The fraction of substrate metabolized (fm ) can be used to estimate drug interactions and can be determined by comparison of the intrinsic clearances (CLint ) of victim drugs obtained from inhibited and uninhibited hepatic enzymes. Commercially available human liver microsomes were recently developed in which one cytochrome P450 (P450) isoform is selectively inactivated. These inactivated liver microsomes were used to evaluate the roles of P450 2C isoforms in the depletion and oxidation of probe substrates...
November 14, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29133569/efficacy-of-tilorone-dihydrochloride-against-ebola-virus-infection
#19
Sean Ekins, Mary A Lingerfelt, Jason E Comer, Alexander N Freiberg, Jon C Mirsalis, Kathleen O'Loughlin, Anush Harutyunyan, Claire McFarlane, Carol E Green, Peter B Madrid
Tilorone dihydrochloride (tilorone) is a small-molecule, orally bioavailable drug that is used clinically as an antiviral outside of the US. A machine learning model trained on anti-Ebola virus (EBOV) screening data previously identified tilorone as a potent in vitro EBOV inhibitor, making it a candidate for the treatment of Ebola virus disease (EVD). In the present study, a series of in vitro ADMET (absorption, distribution, metabolism, excretion, toxicity) assays demonstrated the drug has excellent solubility, high Caco-2 permeability, was not a P-glycoprotein substrate and had no inhibitory activity against five human CYP450 enzymes (3A4, 2D6, 2C19, 2C9 and 1A2)...
November 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29120380/in-vitro-phase-i-metabolism-of-crv431-a-novel-oral-drug-candidate-for-chronic-hepatitis-b
#20
Daniel J Trepanier, Daren R Ure, Robert T Foster
The cytochrome P450-mediated Phase I in vitro metabolism of CRV431 was studied using selective chemical inhibition and recombinant human enzymes. Additionally, the metabolic profile of CRV431 in human, rat, and monkey liver microsomes was investigated. Liver microsomes were incubated for 0-80 min with CRV431, and the metabolite profile was assessed by electrospray ionization liquid chromatography mass spectrometry (ESI-LCMS). CRV431 was extensively metabolized through oxidation to produce various hydroxylated and demethylated species...
November 9, 2017: Pharmaceutics
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