Targeting the pregnane X receptor using microbial metabolite mimicry
نویسندگان
چکیده
منابع مشابه
Activation of pregnane X receptor inhibits
Received 8 August 2012 Revised 7 November 2012 Accepted 2 December 2012 Published Online First 5 January 2013 ABSTRACT Objective To assess the antifibrotic effects of pregnane X receptors (PXRs) in experimental dermal fibrosis. Methods The antifibrotic effects of PXR activation by 5-pregnen-3β-ol-20-one-16α-carbonitrile (PCN) were studied in the bleomycin model for prevention of dermal fibrosis...
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The pregnane X receptor (PXR) is a ligand-activated transcription factor regulating genes central to drug and hormone metabolism in the liver. Previous reports indicated that PXR is expressed in PBMC, but the role of PXR in immune cells remains unknown. In this paper, we report increased PXR expression in mouse and human T lymphocytes upon immune activation. Furthermore, pharmacologic activatio...
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The steroid and xenobiotic-responsive human pregnane X receptor (PXR) binds a broad range of structurally diverse compounds. The structures of the apo and ligand-bound forms of PXR are very similar, in contrast to most promiscuous proteins that generally adapt their shape to different ligands. We investigated the structural origins of PXR's recognition promiscuity using computational solvent ma...
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W e have a love–hate relationship with cholesterol. On one hand, cholesterol is an essential component of cell membranes and serves as the precursor to steroid hormones and bile acids. On the other hand, cholesterol can clog blood vessels and give rise to cardiovascular disease. Moreover, oxidized metabolites of cholesterol, termed oxysterols, are cytotoxic in a variety of different cell types ...
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Sophora flavescens (SF) is an herbal medicine widely used for the treatment of viral hepatitis, cancer, viral myocarditis, gastrointestinal hemorrhage, and skin diseases. It was recently reported that SF up-regulates CYP3A expression. The mechanism of SF-induced CYP3A expression is unknown. In the current study, we tested the hypothesis that SF-induced CYP3A expression is mediated by the activa...
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ژورنال
عنوان ژورنال: EMBO Molecular Medicine
سال: 2020
ISSN: 1757-4676,1757-4684
DOI: 10.15252/emmm.201911621