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  • PRODUCTS
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Related Articles: CAR

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Correlation Between Cytochrome P450 Inducers and Nuclear Receptor Activation – a Screening Approach

View Full Size Research conducted by: Shantanu Roychowdhury (1); Casidy M. Ward (1); Kevin J. Kennedy (1); & Yong Zhao (1) (1) Eurofins Discovery, 6 Research Park Drive, St. Charles, MO 63304 Date of Publication: 2019 Presented at: ISSX 2019 in Portland, OR

Posted in New Publications, Posters | Tagged AhR, CAR, cyp450 inducer, cytochrome p450, PXR | Comments Off on Correlation Between Cytochrome P450 Inducers and Nuclear Receptor Activation – a Screening Approach

Sedaxane—Use of Nuclear Receptor Transactivation Assays, Toxicogenomics, and Toxicokinetics as Part of a Mode of Action Framework for Rodent Liver Tumors

ABSTRACT Experimental data demonstrate a mode of action (MOA) for liver tumors in male rats and mice treated with sedaxane that starts with activation of CAR, followed by altered expression of CAR-responsive genes, increased cell proliferation, and eventually clonal expansion of preneoplastic cells, leading to the development of altered foci and tumors. This MOA isRead More

Posted in New Publications | Tagged AhR, CAR, constitutive androstane receptor, liver tumor, ortholog, PPARa, PPARα, PXR, sedaxane | Comments Off on Sedaxane—Use of Nuclear Receptor Transactivation Assays, Toxicogenomics, and Toxicokinetics as Part of a Mode of Action Framework for Rodent Liver Tumors

Profiling Drug Activity of Human and Ortholog Xenobiotic-Sensing Receptors: PXR, CAR, AhR, and FXR

View Full Size Research conducted by: Koji Toyokawa (1), Ewa Maddox (1), Jack Vanden Huevel (1,2), & Bruce Sherf (1) (1) INDIGO Biosciences, Inc., 1981 Pine Hall Rd, State College, PA, USA (2) Center for Molecular Toxicology and Carcinogenesis, 325 Life Sciences Building, Penn State University, University Park, PA 16802, USA Date of Publication: 2017

Posted in New Publications, Posters | Tagged AhR, CAR, drug activity, FXR, ortholog, PXR, SOT 2017 | Comments Off on Profiling Drug Activity of Human and Ortholog Xenobiotic-Sensing Receptors: PXR, CAR, AhR, and FXR

Differential modulation of FXR activity by chlorophacinone and ivermectin analogs

ABSTRACT Chemicals that alter normal function of farnesoid X receptor (FXR) have been shown to affect the homeostasis of bile acids, glucose, and lipids. Several structural classes of environmental chemicals and drugs that modulated FXR transactivation were previously identified by quantitative high-throughput screening (qHTS) of the Tox21 10 K chemical collection. In the present study, weRead More

Posted in New Publications | Tagged CAR, FXR, LXR, LXRα | Comments Off on Differential modulation of FXR activity by chlorophacinone and ivermectin analogs

Mouse Liver Tumor Mode of Action: Use of Toxicogenomics in Weight of Evidence for Human Relevance Assessment

ABSTRACT The Use of Toxicogenomics in Chemical Safety Testing Current safety testing is geared to produce and accept descriptive data from high-dose animal studies Interpretation of this information has effectively protected our health and safety for decates; however, hindered by lack of understanding mechanistic information Concern over chemical safety for humans and the environment hasRead More

Posted in New Publications | Tagged CAR, PXR | Comments Off on Mouse Liver Tumor Mode of Action: Use of Toxicogenomics in Weight of Evidence for Human Relevance Assessment

Effects of Munitions Compounds on Xenobiotic-Activated Nuclear Receptors and Signaling Pathways

ABSTRACT Exposure to certain munitions compounds is know to alter physiological functions in test organisms, however little is known about their molecular and cellular effects. Several nuclear receptors are regulated by xenobiotic compounds. These nuclear receptors belong to a class of ligand-activated transcription factors that, when heterodimerized with RXRa and bound to their respective DNARead More

Posted in New Publications | Tagged CAR, FXR, LXR, PPAR | Comments Off on Effects of Munitions Compounds on Xenobiotic-Activated Nuclear Receptors and Signaling Pathways

Indigo Announces In Vitro Toxicology Platform

In vitro toxicology platform provides predictive model of liver toxicity.  Aims to reduce the high rates of drug­-induced liver damage State College, PA (May 4, 2016) INDIGO Biosciences, the recognized industry leader in nuclear receptor research, has completed development of an in vitro toxicology platform, meeting the demand for predictive liver toxicity models.  INDIGO’s inRead More

Posted in press | Tagged AhR, CAR, In Vitro Toxicology, LRH-1, LXR, Nrf2, PPAR, PXR | Comments Off on Indigo Announces In Vitro Toxicology Platform

Oxysterols are agonist ligands of RORγt and drive Th17 cell differentiation

ABSTRACT The RAR-related orphan receptor gamma t (RORγt) is a nuclear receptor required for generating IL-17–producing CD4+ Th17 T cells, which are essential in host defense and may play key pathogenic roles in autoimmune diseases. Oxysterols elicit profound effects on immune and inflammatory responses as well as on cholesterol and lipid metabolism. Here, we describe the identification of several naturally occurringRead More

Posted in New Publications | Tagged CAR, er, FXR, GR, PPAR, PPARα, PPARβ, PPARγ, ROR, RORγ, RORγt | Comments Off on Oxysterols are agonist ligands of RORγt and drive Th17 cell differentiation

Evidence for triclosan-induced activation of human and rodent xenobiotic nuclear receptors

 ABSTRACT The bacteriostat triclosan (2,4,4′-trichloro-2′-hydroxydiphenylether) (TCS) decreases rat serum thyroxine via putative nuclear receptor (NR) interaction(s) and subsequent transcriptional up-regulation of hepatic catabolism and clearance. However, due to the evolutionary divergence of the constitutive androstane and pregnane-X receptors (CAR, PXR), TCS-mediated downstream effects may be species-dependent. To test the hypothesis that TCS activates xenobiotic NRsRead More

Posted in New Publications | Tagged CAR, PXR | Leave a comment
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