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Citations Search

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Sci. Rep. 9(1), 4863. Effect of Spheroidal Age on Sorafenib Diffusivity and Toxicity in a 3D HepG2 Spheroid Model. 2019

Eilenberger, C., Rothbauer, M., Ehmoser, E.K., Ertl, P., and Küpcü, S.

Notes: These authors evaluated the impact of spheroid age on drug efficacy screening to better understand variability from lab to lab when using similar models. HepG2 spheroids were established and evaluated for parameters including viability and CYP3A4 activity over an 18-day period. (5210)

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SLAS Discov 24(7):745-754, 745-754. Evaluation of Luminogenic Substrates as Probe Substrates for Bacterial Cytochrome P450 Enzymes: Application to Mycobacterium tuberculosis. 2019

Ortega Ugalde, S., Ma, D., Cali, J.J., and Commandeur, J.N.M.

Notes: Pro-luciferin substrates were evaluated as substrates for Mycobacterium tuberculosis cytochrome P450 enzymes to support applicability for high-throughput screening. (5206)

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Stem Cell Res. 38, 101467. Generation of induced pluripotent stem cells-derived hepatocyte-like cells for ex vivo gene therapy of primary hyperoxaluria type 1. 2019

Estève, J., Blouin, J.M., Lalanne, M., Azzi-Martin, L., Dubus, P., Bidet, A., Harambat, J., Llanas, B., Moranvillier, I., Bedel, A., Moreau-Gaudry, F., and Richard, E.

Notes: The generation of patient-derived induced pluripotent stem cells with additional gene therapy is described. Cytochrome P450 activity assays were performed to determine the functionality of the iPSCs. (5209)

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Cell Metab. 30(2), 374-384. Modeling Steatohepatitis in Humans with Pluripotent Stem Cell-Derived Organoids. 2019

Ouchi, R., Togo, S., Kimura, M., Shinozawa, T., Koido, M., Koike, H., Thompson, W., Karns, R.A., Mayhew, C.N., McGrath, P.S., McCauley, H.A., Zhang, R.R., Lewis, K., Hakozaki, S., Ferguson, A., Saiki, N., Yoneyama, Y., Takeuchi, I., Mabuchi, Y., Akazawa, C., Yoshikawa, H.Y., Wells, J.M., and Takebe, T.

Notes: Multicellular human iPSC liver organiods were generated and assessed using methods including cell viability and CYP3A4 activity assays. (5208)

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Oncotarget 10(32), 3051-3065. Thyroid hormones induce doxorubicin chemosensitivity through enzymes involved in chemotherapy metabolism in lymphoma T cells. 2019

Díaz Flaqué, M.C., Cayrol, M.F., Sterle, H.A., Del Rosario Aschero, M., Díaz Albuja, J.A., Isse, B., Farías, R.N., Cerchietti, L., Rosemblit, C., and Cremaschi, G.A.

Notes: These researchers demonstrated that thyroid hormones induce CYP3A4 metabolic activity, and this modulation may regulate the metabolism of a chemotherapeutic agent. (5211)

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J. Pharmacol. Toxicol. Methods 92, 77-94. mRNA transfection retrofits cell-based assays with xenobiotic metabolism. 2018

DeGroot, D.E., Swank, A., Thomas, R.S., Strynar, M., Lee, M.Y., Carmichael, P.L., and Simmons, S.O.

Notes: The ten most common human liver cytochrome P450 enzymes were introduced into a HEK293T cell line to support the creation of high throughput screening assays. Luminogenic substrates for the P450 enzymes were used to assess activity. (5212)

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18(5), 1085. Assembly of Hepatocyte Spheroids Using Magnetic 3D Cell Culture for CYP450 Inhibition/Induction 2017

Desai, P.K., Tseng, H. and Souza, G.R.

Notes: Spheroid cultures were created from primary hepatocytes by the use of magnetic nanoparticles and magnetization. Hepatocyte spheroid cultures were treated with CYP-inducing or -inhibiting drugs for 72 hours. The media was removed and spheroid cell cultures washed, then luciferin pro-substrates (Promega) added, with the substrate used dependent on the treatment. After a 2-hour incubation, media was removed and aliquoted to new white-walled plates, and an equal volume of Luciferin Detection Reagent was added. At the same time, CellTiter-Glo™ Cell Viability Reagent was added to the original plates in an equal volume. All plates were incubated for 20 minutes before reading in a plate-based luminometer. (4872)

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18, 1085. Assembly of Hepatocyte Spheroids Using Magnetic 3D Cell Culture for CYP450 Inhibition/Induction. 2017

Desai, P. K., Tseng, H. and Souza, G. R. 

Notes: CYP450 activity was measured using the P450-Glo™ Assays for CYP3A4, CYP2B6 and CYP1A2, and viability was measured using two separate luminescent assays, one of which being CellTiter-Glo® Cell Viability Assay. (4877)

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Nat. Commun. 6, 8089. Synergistic activation of human pregnane X receptor by binary cocktails of pharmaceutical and environmental compounds 2015

Delfosse, V., Dendele, B., Huet, T., Grimaldi, M.,  Boulahtouf, A., Gerbal-Chaloin, S., Beucher, B., Roecklin, D., Muller, C., Rahmani, R., Cavaillès, V., Daujat-Chavanieu, M., Vivat, V., Pascussi, J-M., Balaguer, P. and Bourguet, W.

Notes: Humans are exposed to a cocktail of low-dose chemicals in the environment, through diet, and through medication. However, most studies looking at compound toxicity, look at these compounds in isolation, not as they might be encountered in the environment—in mixtures. The pregnane X receptor (PXR) is a xenoreceptor that has been identified by the US Environmental Protection Agency as a major target of environmental and dietary chemicals, and many studies have highlighted the role of nuclear receptors like PXR in transducing the deleterious effects of endocrine disrupting compounds in the environment. The authors of this study used compound screening and functional analysis to demonstrate that the combined use of an environmentally persistent organochlorine pesticide and the active component of contraceptive pills (17α-ethinylestradiol) produces synergistic effects on PXR and expression of its target gene, the cytochrome P450 gene, CYP34A. Gene expression of CYP3A4 was measured using a luciferase reporter created in a pGL3-basic backbone. Activity of the CYP3A4 protein was measured in primary human hepatocytes using the P450-Glo™ CYP3A4 Assay with Luciferin-IPA, and cell number was normalized using the CellTiter-Glo® Luminescent Cell Viability Assay. (4579)

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Assay Drug Dev. Technol. , epub ahead of print. Assessment of Compound Hepatotoxicity Using Human Plateable Cryopreserved Hepatocytes in a 1,536-well-plate Format. 2011

Moeller, T.A., Shukla, S.J. and Xia, M.

Notes: Here the authors describe development of an HTS cell viability assay protocol for use with cultured cyropreserved human primary hepatocytes. Cryopreserved hepatocytes for culturing were prepared as suspensions and dispensed at 2,000 or 4,000 cells/5µl/well in collagen I-coated 1,536-well plates. Cells were allowed to attach and then 23nl of each test compound was added in a dilution series from 2.8nM to 92µM, and cells incubated for 24 or 40 hours. Five microliters of CellTiter-Glo® Reagent was added and cells were incubated 30 minutes before reading the luminescent output. IC50 values for 12 compounds were determined; a summary of the protocol is provided in Table 1 of the paper. Cultured cryopreserved hepatocytes were assayed for function using the P450-Glo® CYP3A4 assay with the Luciferin-IPA substrate. (4182)

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Expert Opin. Drug Metab. Toxicol. 4, 103–120. Bioluminescent assays for ADMET 2008

Cali, J.J., Niles, A., Valley, M.P., O’Brien, M.A., Riss, T.L., and Shultz, J.

Notes: The authors of this review article highlight the use of bioluminescence as a readout for high-throughput ADME/Tox assays. They discuss three strategies for designing bioluminescent assays, using either luciferase, ATP or luciferin substrates as the limiting reagents for a luciferase-catalyzed reaction. Reporter gene assays limit the production of luciferase by tying it to a promoter or DNA regulatory region of interest. Such assays can be used to study genes that are regulated by drugs and other xenobiotics. Bioluminescent assays in which ATP is the limiting reagent of the luciferase reaction can be designed to monitor cell viability or the activity kinases. Bioluminescent assays in which the substrate is limiting can be designed so that the activity of a particular enzyme results in the production of a luciferin substrate that can, in turn, be acted upon by luciferase. (3926)

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Assay Drug Dev. Technol. 5, 127–136. Bioluminescent assays for high-throughput screening 2007

Fan, F. and Wood, K.V.

Notes: The authors of this paper review bioluminescent assay technologies, discussing HTS reporter, cell-based and luciferase biosensor assays. They divide luminescent assays into three basic categories: assays that measure ATP concentration (cell viability and kinase assays), assays that measure changes in luciferase levels (reporter assays, GPCR assays), and assays that measure changes in luciferin levels (protease [including caspase], P450 and MAO assays). (3737)

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Drug Metab. Dispos. 33, 38–48. High volume bioassays to assess Cyp3A4-mediated drug interactions: Induction and inhibition in a single cell line. 2005

Yueh, M.F., Kawahara, M. and Raucy, J.

Notes: A CYP3A4 response element consisting of proximal and distal enhancer sequences with the CYP3A4 promoter was cloned into a pGL3 vector and used in transfection studies with HepG2 cells. The effects of either or both enhancer motifs on luciferase expression were studied in relation to various xenochemical treatments. The researchers also used the P450-Glo™ CYP3A4 Assay to analyze increases in CYP3A4 activities in a stably transfected cell line (DPX-2) and on primary hepatocytes. For these assays, the researchers incubated cells in 96-well or 24-well plates with or without CYP3A4 inhibitors and the P450-Glo™ CYP3A4 substrate. Following a 3 hour incubation, the P450-Glo™ Detection Reagent was added and the luminescence was recorded. In these studies cells were also pretreated with various chemicals including 10µM rifampicin, 1000µM phenobarbital, 100µM dexamethasone, 50µg/ml kava, 50µM methoxychlor, 50µM troglitazone, 100µM omeprazole, 100µM 2-acetylaminofluorene, and 25 µM chrysin. (3221)

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Molecular Imaging 4, 88-90. Visualizing Drug Efficacy In Vivo 2005

Zhang, W., Chen, M., West, D.B. and Purchio, A.F.

Notes: The authors of this paper present proof-of-concept experiments showing that drug metabolism enzyme activity can be measured in whole animals (in vivo) in real time. Using a mouse that expresses a luciferase transgene at constitutively high levels in the liver, the authors evaluated CYP3A4 and CYP3A7 activity using a CYP3A P450 substrate (proluciferin substrate) that is converted into a luciferase substrate by CYP34 activity. The luciferase substrate produced by the P450 activity is then used by luciferase in a reaction that produces light. An increase in luminescence correlates with an increase in enzyme activity in this assay. The authors conclude that optical imaging of reporter mice will provide a new method for looking at drug actions in whole animals, with the caveat that the solubility of the proluciferin substrate is optimized and toxicity is minimized. (3996)

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