keyword
MENU ▼
Read by QxMD icon Read
search

CYP1A1

keyword
https://www.readbyqxmd.com/read/28222316/discovery-and-characterization-of-novel-cyp1b1-inhibitors-based-on-heterocyclic-chalcones-overcoming-cisplatin-resistance-in-cyp1b1-overexpressing-lines
#1
Neill J Horley, Kenneth J M Beresford, Tarun Chawla, Glen J P McCann, Ketan C Ruparelia, Linda Gatchie, Vinay R Sonawane, Ibidapo S Williams, Hoon L Tan, Prashant Joshi, Sonali S Bharate, Vikas Kumar, Sandip B Bharate, Bhabatosh Chaudhuri
The structure of alpha-napthoflavone (ANF), a potent inhibitor of CYP1A1 and CYP1B1, mimics the structure of chalcones. Two potent CYP1B1 inhibitors 7k (DMU2105) and 6j (DMU2139) have been identified from two series of synthetic pyridylchalcones. They inhibit human CYP1B1 enzyme bound to yeast-derived microsomes (Sacchrosomes™) with IC50 values of 10 and 9 nM, respectively, and show a very high level of selectivity towards CYP1B1 with respect to the IC50 values obtained with CYP1A1, CYP1A2, CYP3A4, CYP2D6, CYP2C9 and CYP2C19 Sacchrosomes™...
February 9, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28213913/application-of-crs-pcr-rflp-to-identify-cyp1a1-gene-polymorphism
#2
Mingcui Ding, Xiaoran Duan, Xiaolei Feng, Pengpeng Wang, Wei Wang
BACKGROUND: Cytochrome P4501A1 (CYP1A1) is a member of the cytochrome P450 gene family and plays an important role in the metabolism of exogenous and endogenous material. In recent research, it has been shown that its genetic polymorphisms are associated with many diseases. But the isoschizomers such as the BsrDI enzyme required for the detection of this polymorphism are expensive. METHODS: The study used an improved PCR-RFLP method with mismatched base for detection of the single-nucleotide polymorphism rs1048943...
February 18, 2017: Journal of Clinical Laboratory Analysis
https://www.readbyqxmd.com/read/28212313/chemoprevention-of-rat-mammary-carcinogenesis-by-apiaceae-spices
#3
Farrukh Aqil, Jeyaprakash Jeyabalan, Radha Munagala, Srivani Ravoori, Manicka V Vadhanam, David J Schultz, Ramesh C Gupta
Scientific evidence suggests that many herbs and spices have medicinal properties that alleviate symptoms or prevent disease. In this study, we examined the chemopreventive effects of the Apiaceae spices, anise, caraway, and celery seeds against 17β-estrogen (E2)-mediated mammary tumorigenesis in an ACI (August-Copenhagen Irish) rat model. Female ACI rats were given either control diet (AIN 93M) or diet supplemented with 7.5% (w/w) of anise, caraway, or celery seed powder. Two weeks later, one half of the animals in each group received subcutaneous silastic implants of E2...
February 16, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28201809/newborn-mice-lacking-the-gene-for-cyp1a1-are-more-susceptible-to-oxygen-mediated-lung-injury-and-are-rescued-by-postnatal-%C3%AE-napthoflavone-bnf-administration-implications-for-bronchopulmonary-dysplasia-bpd-in-premature-infants
#4
Paramahamsa Maturu, Yanhong Wei-Liang, Weiwu Jiang, Lihua Wang, Krithika Lingappan, Roberto Barrios, Yao Liang, Bhagavatula Moorthy, Xanthi I Couroucli
No abstract text is available yet for this article.
February 13, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28192119/leflunomide-induces-nad-p-h-quinone-dehydrogenase-1-enzyme-via-the-aryl-hydrocarbon-receptor-in-neonatal-mice
#5
Amrit Kumar Shrestha, Ananddeep Patel, Renuka T Menon, Weiwu Jiang, Lihua Wang, Bhagavatula Moorthy, Binoy Shivanna
Aryl hydrocarbon receptor (AhR) has been increasingly recognized to play a crucial role in normal physiological homeostasis. Additionally, disrupted AhR signaling leads to several pathological states in the lung and liver. AhR activation transcriptionally induces detoxifying enzymes such as cytochrome P450 (CYP) 1A and NAD(P)H quinone dehydrogenase 1 (NQO1). The toxicity profiles of the classical AhR ligands such as 3-methylcholanthrene and dioxins limit their use as a therapeutic agent in humans. Hence, there is a need to identify nontoxic AhR ligands to develop AhR as a clinically relevant druggable target...
February 10, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28178600/whole-flaxseed-diet-alters-estrogen-metabolism-to-promote-2-methoxtestradiol-induced-apoptosis-in-hen-ovarian-cancer
#6
Anushka Dikshit, Karen Hales, Dale Buchanan Hales
The study reported here demonstrates that a flaxseed-supplemented diet causes ovarian tumors in the laying hen to undergo apoptosis, resulting in a reduction of tumor burden, reducing the frequency and severity of ovarian cancer. We have previously shown in normal ovaries that flaxseed and its components down-regulate ERalpha and alter the expression of enzymes that metabolize estrogen. In this study, we analyzed the effects of the two main components of whole flaxseed, ligan and omega 3 fatty acids on estrogen metabolism and the estrogen receptor in ovarian tumors...
January 23, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/28171546/ahr-cyp1a1-interplay-triggers-lymphatic-barrier-breaching-in-breast-cancer-spheroids-by-inducing-12-s-hete-synthesis
#7
Chi Huu Nguyen, Stefan Brenner, Nicole Huttary, Atanas Georgiev Atanasov, Verena Maria Dirsch, Waranya Chatuphonprasert, Sivio Holzner, Serena Stadler, Juliane Riha, Sigurd Krieger, Rainer de Martin, Zsuzsanna Bago-Horvath, Georg Krupitza, Walter Jäger
No abstract text is available yet for this article.
November 15, 2016: Human Molecular Genetics
https://www.readbyqxmd.com/read/28164573/association-studies-of-cyp1a1-exon7-polymorphism-and-gstm1-interaction-with-esophageal-cancer-risk-a-meta-analysis-in-the-chinese-population
#8
Xin-Ping Chen, Da-Feng Xu, Wei-Hua Xu, Zhi-Chao Ma, Jia Yao, Sheng-Miao Fu
BACKGROUND: Although many epidemiological studies have investigated the CYP1A1 exon7 polymorphism and -GSTM1 interaction with esophageal cancer (EC), definite conclusions cannot be drawn. This study was conducted to explore this association in the Chinese population using meta-analysis. METHODS: Relevant studies were identified from PubMed, Springer Link, Ovid, Chinese Wanfang Data Knowledge Service Platform, Chinese National Knowledge Infrastructure, and Chinese Biology Medicine databases published through August 2015...
September 1, 2016: Clinical Laboratory
https://www.readbyqxmd.com/read/28164497/cytochrome-p450-1a1-cyp1a1-gene-polymorphisms-and-susceptibility-to-breast-cancer-a-meta-analysis-in-the-chinese-population
#9
Hui Wu, Quchang Ouyang, Can Tian, Ning Xie, Min Cao, Zheng-Rong Shui
BACKGROUND: Although various individual studies have evaluated the correlation between cytochrome P450 1A1 (CYP1A1) polymorphisms and breast cancer, the results remain inconclusive. To further evaluate the influence of CYP1A1 polymorphisms on breast cancer risk, we conducted a meta-analysis in the Chinese population. METHODS: Studies were identified using PubMed and Chinese databases through December 2015. Pooled odd ratios (ORs) and 95% confidence intervals (CIs) were used to assess the strengths of these associations...
January 1, 2017: Clinical Laboratory
https://www.readbyqxmd.com/read/28157646/polymorphism-in-xenobiotic-and-estrogen-metabolizing-genes-exposure-to-perfluorinated-compounds-and-subsequent-breast-cancer-risk-a-nested-case-control-study-in-the-danish-national-birth-cohort
#10
Mandana Ghisari, Manhai Long, Durita Mohr Røge, Jørn Olsen, Eva C Bonefeld-Jørgensen
: In the present case-cohort study based on prospective data from Danish women, we aimed to estimate the main effect of polymorphisms in genes known to be involved in the steroid hormone metabolic pathway and xenobiotic metabolism on the risk of developing breast cancer. We also studied a possible effect measure modification between genotypes and levels of serum perfluoroalkylated substances (PFASs) on the risk to breast cancer. We have previously reported a weak association between serum PFASs levels and the risk of breast cancer for this study population of Danish pregnant nulliparous women as well as in a smaller case-control study of Greenlandic women...
January 31, 2017: Environmental Research
https://www.readbyqxmd.com/read/28153842/regional-expression-levels-of-drug-transporters-and-metabolizing-enzymes-along-the-pig-and-human-intestinal-tract-and-comparison-with-caco-2-cells
#11
Stefan F C Vaessen, Marola M H van Lipzig, Raymond H H Pieters, Cyrille A M Krul, Heleen M Wortelboer, Evita van de Steeg
Intestinal transporter proteins and metabolizing enzymes play a crucial role in the oral absorption of a wide variety of drugs. The aim of the current study was to better characterize available intestinal in vitro models by comparing expression levels of these proteins and enzymes between porcine intestine, human intestine and Caco-2 cells. We therefore determined the absolute protein expression of 19 drug transporters and the mRNA expression of 12 metabolic enzymes along the pig intestinal tract (duodenum, jejunum, ileum; N=4), in human intestine (jejunum; N=9) and Caco-2 cells...
February 2, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28146477/feedback-control-of-ahr-signalling-regulates-intestinal-immunity
#12
Chris Schiering, Emma Wincent, Amina Metidji, Andrea Iseppon, Ying Li, Alexandre J Potocnik, Sara Omenetti, Colin J Henderson, C Roland Wolf, Daniel W Nebert, Brigitta Stockinger
The aryl hydrocarbon receptor (AHR) recognizes xenobiotics as well as natural compounds such as tryptophan metabolites, dietary components and microbiota-derived factors, and it is important for maintenance of homeostasis at mucosal surfaces. AHR activation induces cytochrome P4501 (CYP1) enzymes, which oxygenate AHR ligands, leading to their metabolic clearance and detoxification. Thus, CYP1 enzymes have an important feedback role that curtails the duration of AHR signalling, but it remains unclear whether they also regulate AHR ligand availability in vivo...
February 9, 2017: Nature
https://www.readbyqxmd.com/read/28139960/development-of-an-in-vitro-model-to-screen-cyp1b1-targeted-anticancer-prodrugs
#13
Zhiying Wang, Yao Chen, Laura M Drbohlav, Judy Qiju Wu, Michael Zhuo Wang
Cytochrome P450 1B1 (CYP1B1) is an anticancer therapeutic target due to its overexpression in a number of steroid hormone-related cancers. One anticancer drug discovery strategy is to develop prodrugs specifically activated by CYP1B1 in malignant tissues to cytotoxic metabolites. Here, we aimed to develop an in vitro screening model for CYP1B1-targeted anticancer prodrugs using the KLE human endometrial carcinoma cell line. KLE cells demonstrated superior stability of CYP1B1 expression relative to transiently transfected cells and did not express any appreciable amount of cognate CYP1A1 or CYP1A2, which would have compromised the specificity of the screening assay...
December 2016: Journal of Biomolecular Screening
https://www.readbyqxmd.com/read/28126315/identification-of-cytochrome-p450-isoforms-involved-in-the-metabolism-of-syl930-a-selective-s1pr1-agonist-acting-as-a-potential-therapeutic-agent-for-autoimmune-encephalitis
#14
Jiaqi Mi, Manman Zhao, Shu Yang, Yufei Jia, Yan Wang, Baolian Wang, Jing Jin, Xiaojian Wang, Qiong Xiao, Jinping Hu, Yan Li
Syl930 is a novel sphingosine-1-phosphate receptor subtype 1 (S1PR1) agonist for the treatment of autoimmune encephalitis with promising receptor selectivity and little risk of bradycardia. Syl930 could be reversibly converted to its phosphorylated metabolite, acting as the active form to provide therapeutic effects, but eliminated principally in the form of oxidative metabolites. The aim of the present study was to identify the cytochrome P450 isoforms (CYPs) responsible for the oxidative metabolism of Syl930...
July 14, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28118673/an-appraisal-of-drug-drug-interactions-with-green-tea-camellia-sinensis
#15
Ahmed A Albassam, John S Markowitz
This review summarizes published in vitro, animal, and clinical studies investigating the effects of green tea (Camellia sinensis) extract and associated catechins on drug-metabolizing enzymes and drug transporters. In vitro studies suggest that green tea extract and its main catechin, (-)-epigallocatechin-3-gallate, to varying degrees, inhibit the activity of CYP1A1, CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2D6, and CYP3A4. UGT1A1 and UGT1A4 isoforms were also inhibited by (-)-epigallocatechin-3-gallate. Animal studies suggest green tea extract and/or (-)-epigallocatechin-3-gallate significantly increase the bioavailability of diltazem, verapamil, tamoxifen simvastatin, 5-fluorouracil, and nicardipine...
January 24, 2017: Planta Medica
https://www.readbyqxmd.com/read/28116098/cyp1b1-mediated-suppression-of-lymphoid-progenitors-in-bone-marrow-by-polycyclic-aromatic-hydrocarbons-coordinately-impacts-spleen-and-thymus-a-selective-role-for-the-ah-receptor
#16
Michele Campaigne Larsen, Alhaji U N'Jai, David L Alexander, Catherine M Rondelli, E C Forsberg, Charles J Czuprynski, Colin R Jefcoate
Bone marrow (BM) hematopoietic stem cells differentiate to common lymphoid progenitors (CLP) that emigrate to the thymus to form T cells or differentiate into immature B cells that then migrate to the spleen for maturation. Rapid in vivo suppression of BM progenitor cells by a single oral or intraperitoneal dose of 7,12-dimethylbenz(a)anthracene (DMBA) subsequently decreased mature lymphoid populations in BM, spleen, and thymus. These suppressions depended on BM CYP1B1, but not on aryl hydrocarbon receptor (AhR) activity...
August 2016: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28115069/diallyl-trisulfide-attenuated-n-hexane-induced-neurotoxicity-in-rats-by-modulating-p450-enzymes
#17
Shuo Wang, Ming Li, Xujing Wang, Xianjie Li, Hongyin Yin, Lulu Jiang, Wenting Han, Gleniece Irving, Tao Zeng, Keqin Xie
Chronic exposure to n-hexane can induce serious nerve system impairments without effective preventive medicines. Diallyl trisulfide (DATS) is a garlic-derived organosulfur compound, which has been demonstrated to have many beneficial effects. The current study was designed to evaluate whether DATS could restrain n-hexane induced neurotoxicity in rats and to explore the underlying mechanisms. Rats were treated with n-hexane (3 g/kg, p.o.) and different doses of DATS (10, 20 and 30 mg/kg, p.o.) for 8 weeks...
January 20, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28109655/the-use-of-rockfish-sebastiscus-marmoratus-as-a-sentinel-species-to-assess-petroleum-hydrocarbons-pollution-a-case-study-in-quanzhou-bay-china
#18
Jun Bo, Ronghui Zheng, Weiming Kuang, Fukun Hong, Qing Xie, Yusheng Zhang
To monitor the biological effects of marine pollution, choosing a native fish species and establishing suitable biomarkers are required. In this study, the full-length cDNA of cyp1a1 was cloned from Sebastiscus marmoratus (SM-CYP1A1). Then the dose-response and time-course induction of hepatic CYP1A1 mRNA by the crude oil water-soluble fraction (WSF) were determined. Subsequently, SM-CYP1A1 mRNA was applied to investigate the biological effect of petroleum hydrocarbon pollution in Quanzhou Bay, China. The transcription levels of hepatic CYP1A1 were significantly elevated in fish caged in the polluted sites for 2weeks compared with those of the reference site, which were correlated with the concentrations of petroleum hydrocarbon and polycyclic aromatic hydrocarbon (PAH) in the surface seawaters...
January 18, 2017: Marine Pollution Bulletin
https://www.readbyqxmd.com/read/28104439/up-regulation-of-cyp1a1-and-phase-ii-enzymes-by-5-ring-isomeric-polycyclic-aromatic-hydrocarbons-in-precision-cut-rat-hepatic-slices-importance-of-molecular-shape
#19
Daphnee Pushparajah, Dfv Lewis, Costas Ioannides
The objectives of the present study were two-fold: (a) to evaluate the role of molecular shape on the interaction of polycyclic aromatic hydrocarbons (PAHs) with the Ah receptor and CYP1A1 upregulation, and (b) to evaluate the potential of PAHs to induce epoxide hydrolase and glutathione S-transferase, two major enzymes involved in their metabolism. In order to achieve these objectives, precision-cut rat liver slices were incubated with a range of concentrations of seven 5-ring isomeric PAHs, namely benzo[c]chrysene, benzo[b]chrysene, benzo[g]chrysene, dibenzo[a,j]anthracene, dibenzo[a,c]anthracene, picene and pentacene, for 24h...
January 16, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28103884/aryl-hydrocarbon-receptor-cytochrome-p450%C3%A2-1a1-pathway-mediates-breast-cancer-stem-cells-expansion-through-pten-inhibition-and-%C3%AE-catenin-and-akt-activation
#20
Abdullah Al-Dhfyan, Ali Alhoshani, Hesham M Korashy
BACKGROUND: Breast cancer stem cells (CSCs) are small sub-type of the whole cancer cells that drive tumor initiation, progression and metastasis. Recent studies have demonstrated a role for the aryl hydrocarbon receptor (AhR)/cytochrome P4501A1 pathway in CSCs expansion. However, the exact molecular mechanisms remain unclear. METHODS: The current study was designed to a) determine the effect of AhR activation and inhibition on breast CSCs development, maintenance, self-renewal, and chemoresistance at the in vitro and in vivo levels and b) explore the role of β-Catenin, PI3K/Akt, and PTEN signaling pathways...
January 19, 2017: Molecular Cancer
keyword
keyword
84017
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"