Identification of Modulators That Activate the Constitutive Androstane Receptor From the Tox21 10K Compound Library
نویسندگان
چکیده
منابع مشابه
Profiling of the Tox21 10K compound library for agonists and antagonists of the estrogen receptor alpha signaling pathway
The U.S. Tox21 program has screened a library of approximately 10,000 (10K) environmental chemicals and drugs in three independent runs for estrogen receptor alpha (ERα) agonist and antagonist activity using two types of ER reporter gene cell lines, one with an endogenous full length ERα (ER-luc; BG1 cell line) and the other with a transfected partial receptor consisting of the ligand binding d...
متن کاملCINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor.
Constitutive androstane receptor (CAR) and pregnane X receptor (PXR) are xenobiotic sensors that enhance the detoxification and elimination of xenobiotics and endobiotics by modulating the expression of genes encoding drug-metabolizing enzymes and transporters. Elevated levels of drug-metabolizing enzymes and efflux transporters, resulting from CAR activation in various cancers, promote the eli...
متن کاملCINPA1 Is an Inhibitor of Constitutive Androstane Receptor That Does Not Activate Pregnane X Receptor s
Constitutive androstane receptor (CAR) and pregnane X receptor (PXR) are xenobiotic sensors that enhance the detoxification and elimination of xenobiotics and endobiotics by modulating the expression of genes encoding drug-metabolizing enzymes and transporters. Elevated levels of drug-metabolizing enzymes and efflux transporters, resulting fromCARactivation in various cancers, promote the elimi...
متن کاملQuantitative High-Throughput Identification of Drugs as Modulators of Human Constitutive Androstane Receptor
The constitutive androstane receptor (CAR, NR1I3) plays a key role in governing the transcription of numerous hepatic genes that involve xenobiotic metabolism/clearance, energy homeostasis, and cell proliferation. Thus, identification of novel human CAR (hCAR) modulators may not only enhance early prediction of drug-drug interactions but also offer potentially novel therapeutics for diseases su...
متن کاملCell-Based High-Throughput Screening for Aromatase Inhibitors in the Tox21 10K Library.
Multiple mechanisms exist for endocrine disruption; one nonreceptor-mediated mechanism is via effects on aromatase, an enzyme critical for maintaining the normal in vivo balance of androgens and estrogens. We adapted the AroER tri-screen 96-well assay to 1536-well format to identify potential aromatase inhibitors (AIs) in the U.S. Tox21 10K compound library. In this assay, screening with compou...
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ژورنال
عنوان ژورنال: Toxicological Sciences
سال: 2018
ISSN: 1096-6080,1096-0929
DOI: 10.1093/toxsci/kfy242