The Furan Fatty Acids 11M5 and 11D5 Can Act as Activators of Human Peroxisome Proliferator-Activated Receptor Gamma. [PDF]
Mol Nutr Food ResFuran fatty acids are abundant in food such as fatty fish. Here we show that some of these can bind to and act as activators of the nuclear receptors, peroxisome proliferator‐activated receptor gamma (PPAR‐gamma) and retinoid X receptor (RXR), in human cells.
Pospiech J +5 more
europepmc +2 more sources
Resveratrol as an Inhibitor of Pregnane X Receptor (PXR): Another Lesson in PXR Antagonism
Journal of Pharmacological Sciences, 2014 The pregnane X receptor (PXR) plays a central role in the regulation of metabolism. Only few PXR antagonists have been described and the mechanism of PXR inhibition is mostly hypothetical or believed to be allosteric. Resveratrol is now being discussed as a novel agent that is capable of attenuating the PXR-inducible expression of the CYP3A4 gene ...
Tomas Smutny, Petr Pavek
openaire +4 more sources
Pregnenolone-16α-carbonitrile inhibits rodent liver fibrogenesis via PXR (pregnane X receptor)-dependent and PXR-independent mechanisms [PDF]
Biochemical Journal, 2005 The effect of liver growth stimulation [using the rodent PXR (pregnane X receptor) activator PCN (pregnenolone-16α-carbonitrile)] in rats chronically treated with carbon tetrachloride to cause repeated hepatocyte necrosis and liver fibrogenesis was examined. PCN did not inhibit the hepatotoxicity of carbon tetrachloride.
Carylyn J, Marek +8 more
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Pregnane X Receptor (PXR) at the Crossroads of Human Metabolism and Disease
Current Drug Metabolism, 2013 Pregnane X Receptor (PXR), a member of the nuclear receptor (NR) superfamily, is expressed in liver and intestine, as also in other tissues and cells. PXR is activated by a wide variety of endobiotics, dietary compounds and pharmaceuticals. This nuclear receptor serves as a master transcriptional regulator of CYP3A isozymes, and also regulates a large ...
Koutsounas, I. +3 more
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Role of pregnane X receptor (PXR) in diet‐induced obesity
The FASEB Journal, 2012 Clinical obesity is a complex metabolic disorder that affects 1 in 3 adults. While a high‐fat diet (HFD) causes obesity and insulin resistance, the specific genes that determine sensitivity to obesity are not known. Recent reports suggest that the nuclear receptor pregnane X receptor (PXR), a xenobiotic receptor that defends against toxic agents, may ...
Maxwell Afari Gyamfi +2 more
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The Major Human Pregnane X Receptor (PXR) Splice Variant, PXR.2, Exhibits Significantly Diminished Ligand-Activated Transcriptional Regulation [PDF]
Drug Metabolism and Disposition, 2009 The pregnane X receptor (PXR; PXR.1) can be activated by structurally diverse lipophilic ligands. PXR.2, an alternatively spliced form of PXR, lacks 111 nucleotides encoding 37 amino acids in the ligand binding domain. PXR.2 bound a classic CYP3A4 PXR response element (PXRE) in electrophoretic mobility shift assays, but transfected PXR.2 failed to ...
Yvonne S, Lin +11 more
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Prioritising research on endocrine disruption in the marine environment: a global perspective
Biological Reviews, EarlyView.ABSTRACT A healthy ocean is a crucial life support system that regulates the global climate, is a source of oxygen and supports major economic activities. A vast and understudied biodiversity from micro‐ to macro‐organisms is integral to ocean health.
Patricia I. S. Pinto +23 more
wiley +1 more source
Activation of Pregnane X Receptor (PXR) and Constitutive Androstane Receptor (CAR) by Herbal Medicines [PDF]
The AAPS Journal, 2009 Pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are transcription factors that control the expression of a broad array of genes involved not only in transcellular transport and biotransformation of many drugs, other xenochemicals, and endogenous substances, such as bile acid, bilirubin, and certain vitamins, but also in various ...
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Pregnane X Receptor (PXR), Constitutive Androstane Receptor (CAR), and Benzoate X Receptor (BXR) Define Three Pharmacologically Distinct Classes of Nuclear Receptors [PDF]
Molecular Endocrinology, 2002 AbstractThe NR1I subfamily of nuclear receptors contains a phylogenetically diverse array of receptors related to the mammalian pregnane X receptor (PXR) (NR1I2) and constitutive androstane receptor (CAR) (NR1I3). We have carried out an extensive comparative analysis of this subgroup with representatives from fish, birds, amphibians, and mammals.
Linda B, Moore +7 more
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The Journal of Physiology, EarlyView.Abstract figure legend A summary of the current knowledge around membrane transporter expression in the most widely used in vitro models of human trophoblasts, including primary placental tissue, cancer cell lines and trophoblast stem cells, as well as the techniques to attempt to mimic the human placenta in vivo.
Rhiannon Pass +2 more
wiley +1 more source