TY - JOUR. T1 - Inhibition of intercellular communication and induction of ethoxyresorufin-O-deethylase activity by polychlorobiphenyls, -dibenzo-p-dioxins and -dibenzofurans in mouse hepa1c1c7 cells.. AU - de Haan, L.H.J.. AU - Halfwerk, S.. AU - Hovens, S.E.L.. AU - de Roos, B.. AU - Koeman, J.H.. AU - Brouwer, A.. PY - 1996. Y1 - 1996. U2 - 10.1016/1382-6689(95)00006-2. DO - 10.1016/1382-6689(95)00006-2. M3 - Article. VL - 1. SP - 27. EP - 37. JO - Environmental Toxicology and Pharmacology. JF - Environmental Toxicology and Pharmacology. SN - 1382-6689. ER - ...
Resveratrol has been shown to exhibit cancer-preventive activities in preclinical studies. We conducted a clinical study to determine the effect of pharmacologic doses of resveratrol on drug- and carcinogen-metabolizing enzymes. Forty-two healthy volunteers underwent baseline assessment of cytochrome P450 (CYP) and phase II detoxification enzymes. CYP1A2, CYP2D6, CYP2C9, and CYP3A4 enzyme activities were measured by the metabolism of caffeine, dextromethorphan, losartan, and buspirone, respectively. Blood lymphocyte glutathione S-transferase (GST) activity and GST-π level and serum total and direct bilirubin, a surrogate for UDP-glucuronosyl transferase (UGT) 1A1 activity, were measured to assess phase II enzymes. After the baseline evaluation, study participants took 1 g of resveratrol once daily for 4 weeks. Enzyme assessment was repeated upon intervention completion. Resveratrol intervention was found to inhibit the phenotypic indices of CYP3A4, CYP2D6, and CYP2C9 and to induce the ...
Cytokines are thought to cause the depression of cytochrome P-450 (CYP)-associated drug metabolism in humans during inflammation and infection. We have examined the role of five cytokines, i.e., interleukin-1 beta, interleukin-4, interleukin-6, tumor necrosis factor-alpha, and interferon-gamma, on the expression of CYP1A2, CYP2C, CYP2E1, CYP3A, and epoxide hydrolase in primary human hepatocyte cultures. Steady state P-450 and epoxide hydrolase mRNA levels, as well as ethoxyresorufin-O-deethylase and nifedipine oxidation activities, which are mainly supported by CYP1A1/1A2 and CYP3A, respectively, were measured. Interleukin-1 beta, interleukin-6, and tumor necrosis factor-alpha were found to be the most potent depressors of P-450 enzymes. After 3 days of treatment, both mRNA levels and enzyme activities were depressed, typically by at least 40%, whatever the cytokine and the enzyme considered. Interferon-gamma also suppressed CYP1A2 and CYP2E1 mRNA levels and ethoxyresorufin-O-deethylase activity ...
The effects of many chemicals on cellular processes are governed by their ability to enter the cell, which is in turn a function of the composition of the cells external environment. To examine this relationship, the effect of serum in cell culture medium on the bioavailability of cytochrome P450 1A (CYP1A)-inducing compounds was determined in PLHC-1 (Poeciliopsis lucida hepatocellular carcinoma) cells. The presence of 10% calf serum in the medium increased the EC50 (effective concentration to achieve 50% maximal response) for induction of ethoxyresorufin O-deethylase (EROD) activity by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) 20-fold as compared to treatment in serum-free medium. Measurement of [3H]TCDD uptake and Ah receptor binding indicated that the apparent difference in potencies was a result of decreased bioavailability in the presence of serum, effectively reducing the concentration of TCDD within the cells. Induction of EROD and CYP1A protein in response to treatment with each of ...
Difference in expression of the cholesterol-metabolizing enzyme cytochrome P450 cholesterol 27-hydroxylase in peripheral blood mononuclear cells (PBMC) before and after treatment with naprosyn, celecoxib or diclofenac ...
Cytochrome P-450 CYP1A1: A liver microsomal cytochrome P-450 monooxygenase capable of biotransforming xenobiotics such as polycyclic hydrocarbons and halogenated aromatic hydrocarbons into carcinogenic or mutagenic compounds. They have been found in mammals and fish. This enzyme, encoded by CYP1A1 gene, can be measured by using ethoxyresorufin as a substrate for the ethoxyresorufin O-deethylase activity.
TY - JOUR. T1 - The metabolism of 4,8-DiMeIQx in conventional and germ-free rats. AU - Knize, Mark G.. AU - övervik, Eva. AU - Midtvedt, Tore. AU - Turteltaub, Ken W. AU - Happe, James A.. AU - Gustafsson, Jan Åke. AU - Felton, James S.. PY - 1989/8. Y1 - 1989/8. N2 - The aromatic amine mutagen, [l4C]2-amino-3,4-8-trimethyl-imidazo[4,5-f]quinoxaline (4,8-DiMeIQx), which is derived from cooked food, was administered to conventional and germ-free AGUS rats previously fed either a semi-synthetic diet containing the cytochrome P-450 inducer β-naphtho-flavone (BNF) or a control diet without BNF. The germ-free animals had longer fecal transit times and lower induction of 7-ethoxyresorufin-O-deethylase activity than conventional rats. Induction with BNF caused a greater percentage of the radioactivity to be excreted in the feces of both germ-free and conventional rats. Feeding BNF also caused a 4-fold induction in germ-free and a 24-fold induction in conventional rat intestinal enzyme levels. ...
TY - JOUR. T1 - Computer-generated high-valent iron-oxo and manganese-oxo species with polyoxometalate ligands. T2 - How do they compare with the iron-oxo active species of heme enzymes?. AU - De Visser, Samüel P.. AU - Kumar, Devesh. AU - Neumann, Ronny. AU - Shaik, Sason. PY - 2004/10/25. Y1 - 2004/10/25. N2 - The structure and reactivity of high-valent FeVO and Mn VIO oxidation catalysts containing a polyoxometalate [PW 11O39]7- lacunary ligand (2) have been investigated by a computational study. Calculations have demonstrated there is an intriguing analogy between these species and the active species (1) of the enzyme cytochrome P450 (see scheme).. AB - The structure and reactivity of high-valent FeVO and Mn VIO oxidation catalysts containing a polyoxometalate [PW 11O39]7- lacunary ligand (2) have been investigated by a computational study. Calculations have demonstrated there is an intriguing analogy between these species and the active species (1) of the enzyme cytochrome P450 (see ...
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The aryl hydrocarbon receptor (AhR) is a transcription factor belonging to the Per-ARNT-Sim family of proteins. These proteins sense molecules and stimuli from the cellular/tissue environment, and initiate signaling cascades to elicit appropriate cellular responses. Recent literature suggests an important function of AhR in hematopoietic stem cell (HSC) biology. However, the molecular mechanisms by which AhR signaling regulates HSC functions are unknown. In previous studies, we and others reported that treatment of mice with the AhR agonist 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) compromises the competitive reconstitution of bone marrow (BM) cells into irradiated host animals. Additional studies indicated a requirement for AhR in hematopoietic cells and not marrow microenvironment cells. In this study, we tested the hypothesis that TCDD-mediated phenotypic and functional changes of HSCs are a result of changes in gene expression that disrupt stem cell numbers and/or their migration. TCDD ...
2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD), the prototypic ligand for the aryl hydrocarbon receptor (AhR), promotes tumor formation in some model systems. However, with regard to breast cancer, epidemiological and animal studies are inconclusive as to whether exposure increases tumor incidence or may instead be protective. We have previously reported that mice exposed to TCDD during pregnancy have impaired differentiation of mammary tissue, including decreased branching and poor development of lobuloalveolar structures. Because normal pregnancy-induced mammary differentiation may protect against subsequent neoplastic transformation, we hypothesized that TCDD-treated mice would be more susceptible to chemical carcinogenesis after parturition. To test this, mice were treated with TCDD or vehicle during pregnancy. Four weeks later, 7,12-dimethylbenz[a]anthracene (DMBA) was administered to induce mammary tumor formation. Contrary to our hypothesis, TCDD-exposed parous mice showed a 4-week delay in ...
Diesel exhaust contains numerous toxic substances that show different modes of action such as triggering aryl hydrocarbon receptor (AhR)-mediated pathways. We investigated AhR-mediated activity of exhaust generated by a heavy-duty diesel engine operated with or without iron- or copper/iron-catalyzed diesel particulate filters (DPFs). AhR agonists were quantified using the DR-CALUX reporter gene assay (exposure of cells for 24 h). We found 54-60 ng 2,3,7,8-tetrachlorodibenzo-p-dioxin CALUX equivalents (TCDD-CEQs) per m3 of exhaust in unfiltered samples and 6-16 ng TCDD-CEQ m3 in DPF-treated samples. DPF applications decreased TCDD-CEQ concentrations by almost 90%. Concentrations of known AhR agonists were determined with GC/HRMS and converted to TCDD-CEQ concentrations using compound-specific relative potency values. The analyzed nine polycyclic aromatic hydrocarbons (PAHs) and the 172,3,7,8-chlorinated dibenzodioxins/furans (23,7,8-PCDD/Fs) contributed only marginally (0.6-1.6%) to the total ...
Patients with ER-negative breast tumors are among the most difficult to treat and exhibit low survival rates due, in part, to metastasis from the breast to various distal sites. Aryl hydrocarbon receptor (AHR) ligands show promise as antimetastatic drugs for estrogen receptor (ER)-negative breast cancer. Triple negative MDA-MB-231 breast cancer cells were treated with eight AHR-active pharmaceuticals including 4-hydroxtamoxifen, flutamide leflunomide, mexiletine, nimodipine, omeprazole, sulindac and tranilast, and the effects of these compounds on cell proliferation (MTT assay) and cell migration (Boyden chamber assay) were examined. The role of the AHR in mediating inhibition of MDA-MB-231 cell invasion was investigated by RNA interference (RNAi) and knockdown of AHR or cotreatment with AHR agonists. Lung metastasis of MDA-MB-231 cells was evaluated in mice administered cells by tail vein injection and prometastatic gene expression was examined by immunohistochemistry. We showed that only the proton
TY - JOUR. T1 - Signaling pathway for 2,3,7,8-tetrachlorodibenzo-p-dioxin-induced TNF-α production in differentiated THP-1 human macrophages. AU - Cheon, Hyeon Joo. AU - Woo, Young Seok. AU - Ji, Young Lee. AU - Hee, Sook Kim. AU - Hyun, Jin Kim. AU - Cho, Sungwon. AU - Nam, Hee Won. AU - Sohn, Jeongwon. PY - 2007/8/31. Y1 - 2007/8/31. N2 - 2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD), a prototypic halogenated aromatic hydrocarbon (HAH), is known as one of the most potent toxicants. At least a part of its toxic effects appears to be derived from its ability to induce TNF-α production. However, the signaling pathway of TCDD that leads to TNF-α expression has not been elucidated. In this study, we investigated the signaling mechanism of TCDD-induced TNF-α expression in PMA-differentiated THP-1 macrophages. TCDD induced both mRNA and protein expression of TNF-α in a dose- and time-dependent manner. α-Naphthoflavone (NF), an aryl hydrocarbon receptor (AhR) inhibitor, prevented the TCDD-induced ...
The first aim of this work was to fully characterise the three most environmentally abundant mono-ortho-substituted polychlorinated biphenyls (PCBs; PCB 105, 118 and 156) including a re-evaluation of their putative antagonistic effects on AhR. Secondly, the effects of mixed halogenated compounds, currently not included in the TEQ estimation, were investigated as AhR agonists based on their environmental exposure and potency. Quantitative real-time PCR (qRT-PCR) was used to measure the AhR mediated induction of CYP1A1 mRNA in rat H4IIE and human MCF-7 cells. The three mono-ortho-substituted PCBs were shown to be antagonists of rat and human AhRs, an effect which is not currently included in the TEQ calculation. 2-bromo-3,7,8-trichlorodibenzo-p-dioxin (2-B-3,7,8-TriCDD) was found to be an AhR agonist that was 2-fold more potent than 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD; considered one of the most potent in the environment). The majority of the other tested compounds were found to be within ...
Seven dog cytochromes P450 (P450s) were heterologously expressed in baculovirus-Sf21 insect cells. Of all enzymes examined, CYP1A1 exhibited high 7-ethoxyresorufin O-deethylase activity (low Km enzyme, 1 μM). CYP2B11 and CYP3A12 effectively catalyzed the N1-demethylation and C3-hydroxylation of diazepam (and its derivatives), whereas CYP3A12 and CYP2D15 catalyzed exclusively the N- and O-demethylation, respectively, of dextromethorphan. However, no saturation velocity curves for the N-demethylation of dextromethorphan (up to 500 μM) were achieved, suggesting a high Km for CYP3A12. In contrast to CYP3A12, the CYP2D15-dependent O-demethylation of dextromethorphan was a low Km process (Km = 0.7 μM), similar to that in dog liver microsomes (Km = 2.3 μM). CYP2D15 was also capable of metabolizing bufuralol (1′-hydroxylation), with a Km of 3.9 μM, consistent with that obtained with dog liver microsomes. CYP3A12 was shown to primarily oxidize testosterone at 16α-, 2α/2β-, and 6β-positions. ...
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TY - JOUR. T1 - Mechanism of benzo[a]pyrene-induced Cyp1a-1 gene expression in mouse Hepa 1c1c7 cells. T2 - Role of the nuclear 6 s and 4 s proteins. AU - Merchant, M.. AU - Wang, X.. AU - Kamps, C.. AU - Rosengren, R.. AU - Morrison, V.. AU - Safe, S.. PY - 1992/1. Y1 - 1992/1. N2 - Treatment of wild-type (wt) aryl hydrocarbon (Ah)-responsive mouse Hepa 1c1c7 cells with benzo[a]pyrene (B[a]P) caused a concentration-dependent induction of ethoxyresorufin O-deethylase (EROD) activity. In contrast, B[a]P was inactive as an inducer in Ah nonresponsive class 1 and class 2 mutant cell lines. In parallel experiments, the nuclear fractions from wt cells treated with 10-7 m [3H]B[a]P contained both the 4 s carcinogen binding protein and the 6 s (Ah receptor) complexes, whereas only the 4 s complex was present in the nuclear fraction of the class 2 mutant cells. The results obtained from cotreatment of wt Hepa 1c1c7 cells with 10-6 or 10-7 m B[a]P and 5 × 10-7 or 10-7 m ...
Complete information for AHR gene (Protein Coding), Aryl Hydrocarbon Receptor, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
The aim of the present study was to evaluate the effects on the susceptibility to colorectal cancer (CRC) of genetic polymorphisms in P-glycoprotein (PGP) and the metabolic enzymes cytochrome P450 1A2 (CYP1A2) and flavin-containing monooxygenase 3 (FMO3). We analyzed five single-nucleotide polymorph …
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Effect of gefitinib on CYP mRNAs expression and EROD activity in NSCLC cell lines The baseline transcript levels of had been determined in both sensitive and resistant cell lines selleck chemical MK-0457 by RT PCR and information are summarized in Figure 4A. CYP1A1 and CYP1A2 had been expressed at important levels only in H322, H292 and Calu three cell lines, CYP2D6 was detected in all cell lines, whereas CYP3A4 was undetected. CYP3A5 was present at higher level only in A549 cells. The inducibility of individual CYP genes by gefitinib was then investigated along with the levels of CYP1A1, CYP1A2, CYP2D6 and CYP3A5 mRNAs have been assessed just after treating cells with the drug. After six h, significantly greater gene expression levels of CYP1A1 and CYP1A2 had been observed in all sensitive cell lines. By contrast no substantial modulation of gene expression was observed in resistant cell lines. As a way to evaluate no matter if modulation of the CYP1A1 transcript levels was connected with ...
2,3,7,8-Tetrachlorodibenzo-p-dioxin(TCDD) has previously shown to induce neurotoxicity through intracellular $Ca^{2+}$ increase in rat neurons. In this study we investigated the role and signaling pathway of intracellular $Ca^{2+}$ in TCDD-induced inhibition of neuronal cell proliferation in SK-...
Abstract Background Environmental toxicants, whose actions are often mediated through the aryl hydrocarbon receptor (AhR) pathway, pose risks to the health and well-being of exposed species, including humans. Of particular ...
Способность ферментов биотрансформации ксенобиотиков опухолевой клетки метаболизировать цитостатики может влиять на чувствительность опухоли к химиотерапии и, как следствие, на исход лечения. В биотрансформации препаратов, входящих в стандартные протоколы неоадъювантной химиотерапии, участвуют ферменты суперсемейства цитохромов Р450 (CYP), функциональные свойства которых могут зависеть от уровня экспрессии их генов. В работе определен уровень экспрессии генов цитохромов CYP1В1, CYP2А6, CYP3A4, CYP3A5, CYP2B6, CYP2C8, CYP2C9, CYP2C19 в 62 образцах опухолевой ткани у ...
摘要(Abstract): 采用半静态水体暴露的方式研究了非离子表面活性剂对成熟雄性斑马鱼精巢组织的影响。用荧光定量PCR(qRTPCR)方法检测试验鱼精巢雌激素受体α(ERα)、雄激素受体(AR)基因以及性激素合成相关细胞色素P450酶类基因(CYP17和CYP19a)的表达,通过组织学观察研究受试鱼精巢结构的变化。结果表明,壬基酚聚氧乙烯醚(NPEO)暴露可以引起雄性斑马鱼精巢组织结构的改变,并影响成年雄性斑马鱼ERα、AR基因和性激素合成相关细胞色素P450酶类基因的表达水平,且10.0 mg·L~(-1)的NPEO暴露可以显著上调CYP19a、ERα和AR基因的表达量,可显著下调斑马鱼精巢中CYP17基因的表达量。在组织学上,0.1 mg·L~(-1)组斑马鱼生精小管内不仅生精小囊数目减少,且管腔中精子数量减少,出现非细胞区域; 1.0和10.0 ...
CYP2A6 is the detox enzyme responsible for eliminating nicotine with clear link between CYP2A6 activity & lung cancer risk. Learn more about this enzyme.
Product Name: 1,8-DibromonaphtaleneFormula: C10H6Br2Weight: 285.96264SMILES: BrC1C2C(C=CC=1)=CC=CC=2BrCAS NO: 1137868-96-2 Product: TAK-960 (hydrochloride)
Product Name: 1-bromo-6-phenyl-PyreneFormula: C22H13BrWeight: 357.24262SMILES: C1=CC=C(C=C1)C2=C3C4=C5C(=CC=C4C=C2)C(Br)=CC=C5C=C3CAS NO: 64917-83-5 Product:
CYP2D6-ГЕНОТИПИРОВАНИЕ В ОЦЕНКЕ ЭФФЕКТИВНОСТИ ТЕРАПИИ ТАМОКСИФЕНОМ У БОЛЬНЫХ ГОРМОНОПОЗИТИВНЫМ РАКОМ МОЛОЧНОЙ ЖЕЛЕЗЫ
豊田茂 厚生科学研究班「小児等特殊患者群に対する医薬品の用法 用量の確立に関する研究」平成14年度報告書, 2002 被引用文献1件 ...
TY - JOUR. T1 - Indole scaffolds as a promising class of the aryl hydrocarbon receptor ligands. AU - Dvořák, Zdeněk. AU - Poulíková, Karolína. AU - Mani, Sridhar. N1 - Funding Information: We acknowledge financial support from the Czech Science Foundation [19-00236S]; the student grant from Palack? University in Olomouc [PrF-2021-005]. Funding Information: We acknowledge financial support from the Czech Science Foundation [ 19-00236S ]; the student grant from Palacký University in Olomouc [ PrF-2021-005 ]. Publisher Copyright: © 2021 Elsevier Masson SAS. PY - 2021/4/5. Y1 - 2021/4/5. N2 - The aryl hydrocarbon receptor (AhR), deemed initially as a xenobiotic sensor, plays multiple physiological roles and is involved in various pathophysiological processes and many diseases etiology. Therefore, the therapeutic and chemopreventive targeting of AhR is a fundamental issue. To date, thousands of structurally diverse ligands of AhR have been identified. The bottleneck in targeting the AhR is ...
Bioflavonoids are plant compounds touted for their potential to treat or prevent several diseases including cancers induced by common environmental chemicals. Much of the biologic activity of one such class of pollutants, polycyclic aromatic hydrocarbons (PAH), is mediated by the aryl hydrocarbon receptor/transcription factor (AhR). For example, the AhR regulates PAH immunotoxicity that manifests as pre-B cell apoptosis in models of B cell development. Because bioflavonoids block PAH-induced cell transformation and are structurally similar to AhR ligands, it was postulated that some of them would suppress PAH-induced, AhR-dependent immunotoxicity, possibly through a direct AhR blockade. This hypothesis was tested using a model of B cell development in which pre-B cells are cultured with and are dependent on bone marrow stromal or hepatic parenchymal cell monolayers. Of seven bioflavonoids screened, galangin (3,5,7-trihydroxyflavone) blocked PAH-induced but not C(2)-ceramide- or H(2)O(2)-induced ...
BACKGROUND: Replacing beta-cells by islet-transplantation can cure type 1 diabetes, but up to 70% of beta-cells die within 10 days of transplantation. ARNT (Aryl hydrocarbon Receptor Nuclear Translocator) regulates beta-cell function, and potentially survival. Lack of ARNT impairs the ability of beta-cells to respond to physiological stress and potentiates the onset of diabetes, but the exact role of ARNT in graft outcome is unknown. AIM: To investigate the effect of beta-cell deletion of ARNT on graft outcomes. METHODS: Islets were isolated from donor mice which had beta-cell specific ARNT-deletion (beta-ARNT) or littermate floxed controls. The islets were transplanted into diabetic SCID recipients in ratios of (a) 3 donors: 1 recipient, (b) 1 donor: 1 recipient or (c) (1/2) of the islets from 1 donor: 1 recipient. After 28 days, the kidney containing the graft was removed (nephrectomy) to exclude regeneration of the endogenous pancreas. RESULTS: In the supra-physiological-mass model (3:1), both groups
TY - JOUR. T1 - Ligand-independent activation of the arylhydrocarbon receptor by ETK (Bmx) tyrosine kinase helps MCF10AT1 breast cancer cells to survive in an apoptosis-inducing environment. AU - Fujisawa, Yasuko. AU - Li, Wen. AU - Wu, Dalei. AU - Wong, Patrick. AU - Vogel, Christoph. AU - Dong, Bin. AU - Kung, Hsing Jien. AU - Matsumura, Fumio. PY - 2011/10/1. Y1 - 2011/10/1. N2 - It has been reported that the arylhydrocarbon receptor (AHR) is overexpressed in certain types of breast tumors. However, so far no concrete evidence has been provided yet as to why and how the overexpressed AHR in those cancer cells is functionally activated without exogenous ligands. Here we show that the AHR was functionally activated when estrogen receptor-negative, AHR overexpressing MCF10AT1 human breast cancer cells (designated P20E) were subjected to serum starvation. Transfection of cells with ETK-KQ, a plasmid for kinase-dead epithelial and endothelial tyrosine kinase (ETK), attenuated this AHR activation. ...
TY - JOUR. T1 - Mechanism of action and development of selective aryl hydrocarbon receptor modulators for treatment of hormone-dependent cancers (Review).. AU - Safe, Stephen. AU - McDougal, Andrew. PY - 2002/6. Y1 - 2002/6. N2 - Ligand-activated receptors are extensively used as targets for developing tissue-selective drugs for treatment of multiple diseases including cancers. The aryl hydrocarbon receptor (AhR) is a basic helix-loop-helix transcription factor that binds both synthetic chemicals such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and naturally-occurring phytochemicals, sterols and heme breakdown products. The high affinity ligand TCDD induces several AhR-mediated changes in gene expression, tissue/species-specific toxicities, and both tumorigenic and anticarcinogenic responses including inhibition of estrogen-dependent mammary and uterine tumor formation and growth. Research in this laboratory has demonstrated that TCDD inhibits E2-induced responses in the rodent uterus and ...
TY - JOUR. T1 - Role of AhR/ARNT system in skin homeostasis. AU - Furue, Masutaka. AU - Takahara, Masakazu. AU - Nakahara, Takeshi. AU - Uchi, Hiroshi. PY - 2014/1/1. Y1 - 2014/1/1. N2 - Aryl hydrocarbon receptor (AhR) is a ligand-dependent transcription factor that binds to structurally diverse synthetic and naturally occurring chemicals including dioxins, flavonoids, tryptophan photoproducts, and Malassezia metabolites. Upon binding to its ligands, cytoplasmic AhR translocates to the nucleus, heterodimerizes with aryl hydrocarbon receptor nuclear translocator (ARNT), and mediates numerous biological and toxicological effects by inducing the transcription of various AhR-responsive genes. AhR ligation controls oxidation/antioxidation, epidermal barrier function, photo-induced response, melanogenesis, and innate immunity. This review summarizes recent advances in the understanding of the regulatory mechanisms of skin homeostasis mediated by the AhR/ARNT system.. AB - Aryl hydrocarbon receptor ...
Cheung, YL, Snelling, J, Mohammed, NND, Gray, TJB and Ioannides, C (1996) Interaction with the aromatic hydrocarbon receptor, CYP1A induction, and mutagenicity of a series of diaminotoluenes: Implications for their carcinogenicity ...
6-Formylindolo[3,2-b]carbazole (FICZ) is a potent aryl hydrocarbon receptor (AHR) agonist that is efficiently metabolized by AHR-regulated cytochrome P4501 enzymes. FICZ is a proposed physiological AHR ligand that induces its own degradation as part of a regulatory negative feedback loop. In vitro studies in cells show that CYP1 inhibition in the presence of FICZ results in enhanced AHR activation, suggesting that FICZ accumulates in the cell when its metabolism is blocked. We used zebrafish (Danio rerio) embryos to investigate the in vivo effects of FICZ when CYP1A is knocked down or inhibited. Embryos were injected with morpholino antisense oligonucleotides targeting CYP1A (CYP1A-MO), Ahr2, or a combination of both. FICZ exposure of non-injected embryos or embryos injected with control morpholino had little effect. In CYP1A-MO-injected embryos, however, FICZ dramatically increased mortality, incidence and severity of pericardial edema and circulation failure, reduced hatching frequency, ...
The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that upon activation by the toxicant 2,3,7,8 tetrachlorodibenzo-p-dioxin (TCDD) stimulates gene expression and toxicity. AHR is also important for normal mouse physiology and may play a role in cancer progression in the absence of environmental toxicants. The objective of this report was to identify AHR-dependent genes (ADGs) whose expression is regulated by AHR in the absence of toxicants. RNA-Seq analysis revealed that AHR regulated the expression of over 600 genes at an FDR | 10% in MCF-7 breast cancer cells upon knockdown with short interfering RNA. Pathway analysis revealed that a significant number of ADGs were components of TCDD and tumor necrosis factor (TNF) pathways. We also demonstrated that siRNA knockdown of AHR modulated TNF induction of MNSOD and cytotoxicity in MCF-7 cells. Collectively, the major new findings of this report are: (1) endogenous AHR promotes the expression of xenobiotic metabolizing enzymes
GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes. - Mechanism of Action & Protocol.
This study provides new insights into the mechanisms underlying the carcinogenic effects of tobacco smoke. Multiple genes encoding enzymes (CYP1A1, CYP1B1, AKRs, ALDH3A1, NQO1, and UGTs) involved in carcinogen metabolism were overexpressed in the oral mucosa of smokers. PAHs, an important class of tobacco carcinogen, are likely to mediate some of these expression changes. The AHR, a ligand-activated transcription factor, binds with high affinity to PAHs. Following ligand binding, the AHR translocates to the nucleus where it forms a heterodimer with ARNT. The AHR-ARNT heterodimer then binds to xenobiotic-responsive elements in the upstream regulatory region of target genes, resulting in the transcriptional activation of a network of genes, including CYP1A1 and CYP1B1 (33). The activation of AHR-mediated signaling leading to induction of xenobiotic metabolism provides a first line of defense against environmental carcinogens. However, the induction of xenobiotic-metabolizing enzymes by ...
4940 The arylhydrocarbon receptor (AhR) is a ligand-activated transcription factor regulating transcription of genes encoding primarily drug metabolizing enzymes. Use of its persistent agonists such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and related compounds demonstrated that the AhR mediates species- and tissue-dependent toxicities, including wasting syndrome, immunotoxicty, and carcinogenesis. It has been reported that expression of a constitutively active mutant AhR in transgenic mice resulted in development of stomach tumors, demonstrating the oncogenic potentials of the AhR in gastric cancer. On the other hand, recent reports showed that AhR agonists inhibited pancreatic cancer cell growth and that AhR pathway mediated the effect of antitumor agent in breast tumor cells. To elucidate the functional significance of the AhR pathway in gastric cancer, we examined the expression of AhR in gastric cancer tissues and cell lines and the effect of AhR agonists in gastric cancer cell lines. ...
The ligand-dependent transcription factor aryl hydrocarbon receptor (AhR) has been implicated in various immune functions. Our previous studies have shown that AhR activation by exposure of ovalbumin (OVA)-immunized mice to the potent ligand 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) increases immunization-induced IFN- production in the spleen and suppresses the production of Th2 cytokines and OVA-specific antibodies. In the present study, we used transgenic (Tg) mice that express a constitutively active mutant of aryl hydrocarbon receptor (CA-AhR) specifically in T-lineage cells to clarify the role of AhR activation in T cells in these reactions. The results of this study clearly demonstrated that AhR activation only in the T cells augments IFN- production upon OVA immunization. By contrast, production of Th2 cytokines and antibodies were not significantly suppressed by CA-AhR in the T cells. These results suggest that suppression of Th2 cytokines and antibodies production require AhR ...
AIP (aryl hydrocarbon receptor interacting protein), Authors: Sayka Barry, Márta Korbonits. Published in: Atlas Genet Cytogenet Oncol Haematol.
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Harmine and harmaline are promising candidate to inhibit TCDD-mediated induction of Cyp1a1 in mice hepatic and extrahepatic tissues.
Cytochrome P450 CYP1B1 is a recently cloned dioxin-inducible form of the cytochrome P450 family of xenobiotic metabolizing enzymes. An antibody raised against a peptide specific for CYP1B1 was found to recognize CYP1B1 expressed in human lymphoblastoid cells but not to recognize other forms of cytochrome P450, particularly CYP1A1 and CYP1A2. Using this antibody, the cellular distribution and localization of CYP1B1 were investigated by immunohistochemistry in a range of malignant tumors and corresponding normal tissues. CYP1B1 was found to be expressed at a high frequency in a wide range of human cancers of different histogenetic types, including cancers of the breast, colon, lung, esophagus, skin, lymph node, brain, and testis. There was no detectable immunostaining for CYP1B1 in normal tissues. These results provide the basis for the development of novel methods of cancer diagnosis based on the identification of CYP1B1 in tumor cells and the development of anticancer drugs that are selectively ...
Mouse anti Human ARNT antibody, clone 3D10 recognizes human Aryl hydrocarbon receptor nuclear translocator, also known as ARNT, Class E ba
DESIGN: The test was performed on juvenile fish, which was exposed to Spartakus (concentrations of prochloraz: 0.05; 0.15 and 0.38 mg.L-1) for 28 days. Haematological indices were assessed using unified methods of haematological examination in fish. Plasma biochemical indices were determined by biochemical analyzer. Concentration of total cytochrome P450 (CYP), glutathione (GSH) content and glutathione-S-transferase (GST) activity were determined spectrophotometrically in hepatopancreas. Activity of liver ethoxyresorufin-O-deethylase (EROD) activity was measured spectrofluorimetrically. Ferric reducing ability of plasma (FRAP) and ceruloplasmin activity were assessed spectrophotometrically. Histological changes in samples of hepatopancreas, skin, gills, spleen, head kidney and caudal kidney were examined by light microscopy ...
Principal Investigator:ICHIHARA Sahoko, Project Period (FY):2006 - 2008, Research Category:Grant-in-Aid for Scientific Research (C), Section:一般, Research Field:Hygiene
The human CYP2Cs are an important subfamily of P450 enzymes that metabolize approximately 20% of clinically used drugs. There are four members of the subfamily, CYP2C8, CYP2C9, CYP2C19, and CYP2C18. Of these CYP2C8, CYP2C9, and CYP2C19 are of clinical importance. The CYP2Cs also metabolize some endo …
CYP3A5 is a member of the CYP3A family of genes located on chromosome 7. The CYP3A subfamily of enzymes responsible for the metabolism of more than 50% of medications that undergo hepatic metabolism and first-pass metabolism in intestinal epithelial cells. The CYP3A5 expression level and enzymatic activity can be modulated by genetic variation. CYP3A5 allelic frequency depends upon ethnicity. For example, in individuals of European descent the most common allele is the CYP3A5*3 allele (c.219-237A,G), which results in a splicing defect and absence of enzyme activity. In individuals of African descent, the *1 allele (functional enzyme) is most common. The distribution of CYP3A5*3 allele frequencies ranges from 0.14 among sub-Saharan Africans to 0.95 in European populations.. In general, most drugs metabolized by CYP3A5 are also metabolized by CYP3A4 and usually to a greater degree than CYP3A5. For this reason, substrates of these 2 enzymes are sometimes listed together in publications and ...
enzymes linked to the metabolism and elimination of a variety of exogenous (medication, toxins and carcinogens) and endogenous compounds (steroid hormones). On the whole, stage I biotransformation enzymes, together with People of the cytochrome P450 spouse and children, catalyze reactions that boost the reactivity of Unwanted fat-soluble compounds and prepare them for reactions catalyzed by phase II biotransformation enzymes ...
Covid-19 is the acute illness caused by SARS-CoV-2 with initial clinical symptoms such as cough, fever, malaise, headache, and anosmia. After entry into
Abstract Background Environmental toxicants, whose actions are often mediated through the aryl hydrocarbon receptor (AhR) pathway, pose risks to the health and well-being of exposed species, including humans. Of particular ...
The aryl hydrocarbon receptor (AhR) is a ligand-dependent transcriptional factor widely expressed among immune, epithelial, endothelial and stromal cells in barrier tissues.
Background Malignancy control cells (CSCs) possess increased level of resistance to cancers chemotherapy. possess been mystery, but right here we demonstrate it is definitely an aryl hydrocarbon receptor (AHR) agonist and this takes on a essential part. AHR is definitely a transcription element triggered by 2,3,7,8-tetrachlorodibenzo-value using the Cheng-Prussoff formula [55], where Kis the inhibition continuous for a medication (the contending ligand, i.elizabeth. tranilast or another non-labeled ligand): it represents the focus of the contending ligand in a competition assay which would take up 50% 2226-96-2 supplier of the receptors if no radioligand had been present. T is definitely the focus of free of charge radioligand utilized in the assay, and KD is definitely the dissociation continuous of the radioligand for the receptor. The Ki worth for a contending ligand is definitely an estimation of its presenting identified in an self-employed presenting or practical assay under related ...
, even though the CYP2C19*2 and CYP2C19*3 alleles correspond to lowered metabolism. The CYP2C19*2 and CYP2C19*3 alleles account for 85 of reduced-function
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Polymorphisms in the following genes: ABCB1, ABCG2, COMT, CYP17, CYP19, CYP1B1, CYP1A1, CYP1A2, CYP2C8, CYP2C9, CYP2J2, CYP3A4, CYP3A5, DPYD, EPHX2, ERalpha, ERbeta, ERCC1, ERCC2, GSTP1, HIF1A, MPO, MTHFR, NQO1, p53, PPARD, SLCO1B3, TYMS, UGT1A1, VEGF, VEGFR, EGFR, SLC28A1, CDA, XRCC1, OCT1, OCT2, CHRNA3 and CHRNA5 will be analyzed by the Clinical Pharmacology Program ...
How an organism copes with chemicals is largely determined by the genes and proteins that collectively function to defend against, detoxify and eliminate chemical stressors. This integrative network includes receptors and transcription factors, biotransformation enzymes, transporters, antioxid...
View mouse Cyp4f14 Chr17:32905071-32917342 with: phenotypes, sequences, polymorphisms, proteins, references, function, expression
View mouse Cyp2e1 Chr7:140763739-140774987 with: phenotypes, sequences, polymorphisms, proteins, references, function, expression
Principal nameCYP2C11 antibodyAlternative names for CYP2C11 antibodyCytochrome P450 2C11, CYPIIC11, Cytochrome P450H, Cytochrome P450-UT-ASwissProt…
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