Pregnane X Receptor Is a Target of Farnesoid X Receptor [PDF]
The pregnane X receptor (PXR) is an essential component of the body's detoxification system. PXR is activated by a broad spectrum of xenobiotics and endobiotics, including bile acids and their precursors. Bile acids in high concentrations are toxic; therefore, their synthesis is tightly regulated by the farnesoid X receptor, and their catabolism ...
Diana, Jung +2 more
openaire +2 more sources
The pregnane X receptor (PXR, NR1I2) is a nuclear receptor which exerts its regulatory function by heterodimerization with the retinoid-X-receptor α (RXRα, NR2B1) and binding to the promoter and enhancer regions of diverse target genes.
Juan Pablo Rigalli +3 more
doaj +1 more source
The pregnane X receptor in tuberculosis therapeutics [PDF]
Among the infectious diseases, tuberculosis (TB) remains the second most common cause of death after HIV. TB treatment requires the combination of multiple drugs including the rifamycin class. However, rifamycins are activators of human pregnane X receptor (PXR), a transcription factor that regulates drug metabolism, drug resistance, energy metabolism ...
Amina I, Shehu +3 more
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The protective role of pregnane X receptor in lipopolysaccharide/D-galactosamine-induced acute liver injury. [PDF]
The pregnane X receptor (PXR) is a nuclear receptor transcription factor regulating drug-metabolizing enzymes and transporters that facilitate xenobiotic and endobiotic detoxification.
Damjanov, Ivan +2 more
core +2 more sources
Pregnane X receptor activation potentiates ritonavir hepatotoxicity [PDF]
Ritonavir (RTV) is on the World Health Organization's List of Essential Medicines for antiretroviral therapy, but can cause hepatotoxicity by unknown mechanisms. Multiple clinical studies found that hepatotoxicity occurred in 100% of participants who were pretreated with rifampicin or efavirenz followed by RTV-containing regimens.
Amina I. Shehu +9 more
openaire +2 more sources
The Effects of Pregnenolone 16α-Carbonitrile Dosing on Digoxin Pharmacokinetics and Intestinal Absorption in the Rat [PDF]
The effect of Pgp induction in rats by pregnenolone 16α-carbonitrile (PCN) (3 days, 35 mg/kg/d, p.o.) on digoxin pharmacokinetics and intestinal transport has been assessed.
Anna-Lena Ungell +12 more
core +2 more sources
Resveratrol as an Inhibitor of Pregnane X Receptor (PXR): Another Lesson in PXR Antagonism
.: 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.
Tomas Smutny, Petr Pavek
doaj +1 more source
Unsaturated fatty acid regulation of cytochrome P450 expression via a CAR-dependent pathway. [PDF]
The liver is responsible for key metabolic functions, including control of normal homoeostasis in response to diet and xenobiotic metabolism/detoxification.
Finn, Robert +3 more
core +2 more sources
Realising the therapeutic potential of neuroactive steroid modulators of the GABAA receptor [PDF]
In the 1980s particular endogenous metabolites of progesterone and of deoxycorticosterone were revealed to be potent, efficacious, positive allosteric modulators (PAMs) of the GABAA receptor (GABAAR).
Belelli, Delia +3 more
core +1 more source
Post-translational modification of pregnane x receptor [PDF]
Pregnane x receptor (PXR, NR1I2) was originally characterized as a broad spectrum entero-hepatic xenobiotic 'sensor' and master-regulator of drug inducible gene expression. A compelling description of ligand-mediated gene activation has been unveiled in the last decade that firmly establishes this receptor's central role in the metabolism and transport
Staudinger, Jeffrey Leonard +3 more
openaire +3 more sources

