Phosphorylated Nuclear Receptor CAR Forms a Homodimer To Repress Its Constitutive Activity for Ligand Activation
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چکیده
منابع مشابه
Constitutive and ligand-induced nuclear localization of oxytocin receptor
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متن کاملThe Constitutive Androstane Receptor (CAR): a nuclear receptor in health and disease
Constitutive Androstane Receptor (CAR, NR1I3), a member of the nuclear receptor superfamily of transcription factors, has emerged as one of the key regulators of the drug and xenobiotic metabolism. The unique feature that separates CAR from other members of the superfamily is that it remains active in the absence of ligand and is further regulated by activators. From its first isolation in 1994...
متن کاملActive ERK1/2 protein interacts with the phosphorylated nuclear constitutive active/androstane receptor (CAR; NR1I3), repressing dephosphorylation and sequestering CAR in the cytoplasm.
The nuclear constitutive active/androstane receptor (CAR) is inactivated and sequestered in the cytoplasm when Thr-38 is phosphorylated. Here, we have demonstrated that activated ERK1/2 interacts with phosphorylated CAR to repress dephosphorylation of Thr-38. The phosphorylation-dependent interaction between CAR and ERK1/2 was examined by co-immunoprecipitation experiments of ectopically expres...
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The pregnane X receptor (PXR/SXR, NR1I2) and constitutive androstane receptor (CAR, NR1I3) are nuclear receptors (NRs) involved in the regulation of many genes including cytochrome P450 enzymes (CYPs) and transporters important in metabolism and uptake of both endogenous substrates and xenobiotics. Activation of these receptors can lead to adverse drug effects as well as drug-drug interactions....
متن کاملThe orphan nuclear receptor, DAX-1, functions as a potent co-repressor of the constitutive androstane receptor (CAR, NR1I3)
Regulation of gene transcription is controlled in part by nuclear receptors (NR) that function coordinately with coregulator proteins. The human constitutive androstane receptor (CAR; NR1I3) is primarily expressed in liver and regulates the expression of genes involved in xenobiotic metabolism as well as hormone, energy and lipid homeostasis. In this report, DAX-1, a NR family member with corep...
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ژورنال
عنوان ژورنال: Molecular and Cellular Biology
سال: 2017
ISSN: 0270-7306,1098-5549
DOI: 10.1128/mcb.00649-16