Results 21 to 30 of about 10,479 (197)

Expanding the Library of 1,2,4-Oxadiazole Derivatives: Discovery of New Farnesoid X Receptor (FXR) Antagonists/Pregnane X Receptor (PXR) Agonists

open access: yesMolecules, 2023
Compounds featuring a 1,2,4-oxadiazole core have been recently identified as a new chemotype of farnesoid X receptor (FXR) antagonists. With the aim to expand this class of compounds and to understand the building blocks necessary to maintain the ...
Claudia Finamore   +11 more
doaj   +2 more sources

S-nitrosylation attenuates pregnane X receptor hyperactivity and acetaminophen-induced liver injury [PDF]

open access: yesJCI Insight
Drug-induced liver injury (DILI), especially acetaminophen overdose, is the leading cause of acute liver failure. Pregnane X receptor (PXR) is a nuclear receptor and the master regulator of drug metabolism.
Qi Cui   +13 more
doaj   +2 more sources

Marine Ligands of the Pregnane X Receptor (PXR): An Overview [PDF]

open access: yesMarine Drugs, 2019
Pregnane X Receptor (PXR) is a ligand-activated transcription factor which binds many structurally different molecules. The receptor is able to regulate the expression of a wide array of genes and is involved in cancer and different key physiological ...
Alejandro Carazo   +2 more
doaj   +3 more sources

Pregnane X receptor reduces particulate matter-induced type 17 inflammation in atopic dermatitis [PDF]

open access: yesFrontiers in Immunology
BackgroundEpidemiological evidence suggests that particulate matter (PM) exposure can trigger or worsen atopic dermatitis (AD); however, the underlying mechanisms remain unclear. Recently, pregnane X receptor (PXR), a xenobiotic receptor, was reported to
Ji Su Lee   +17 more
doaj   +2 more sources

CYP3A4 and pregnane X receptor humanized mice [PDF]

open access: yesJournal of Biochemical and Molecular Toxicology, 2007
Marked species differences exist in P450 expression and activities. In order to produce mouse models that can be used to more accurately predict human drug and carcinogen metabolism, P450‐ and xenobiotic receptor humanized mice are being prepared using ...
Gonzalez, Frank J., Frank J. Gonzalez
core   +3 more sources

Pregnane X Receptor Is SUMOylated to Repress the Inflammatory Response [PDF]

open access: yesThe Journal of Pharmacology and Experimental Therapeutics, 2010
Long-term treatment of patients with the macrolide antibiotic and prototypical activator of pregnane X receptor (PXR) rifam-picin (Rif) inhibits the inflammatory response in liver. We show here that activation of the inflammatory response in hepato-cytes
Jeff L. Staudinger, Gang Hu, Chenshu Xu
core   +4 more sources

Pregnane X Receptor Is a Target of Farnesoid X Receptor [PDF]

open access: yesJournal of Biological Chemistry, 2006
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   +4 more sources

Diethylstilbestrol-scaffold-based pregnane X receptor modulators

open access: yesEuropean Journal of Medicinal Chemistry, 2015
Due to its function as a regulator of drug-metabolizing enzymes and transporters, pregnane X receptor (PXR) represents an important factor involved in drug metabolism.
Smodiš, D   +6 more
core   +4 more sources

The constitutive androstane receptor and pregnane X receptor in the brain [PDF]

open access: yesBritish Journal of Pharmacology, 2020
Since their discovery, the orphan nuclear receptors constitutive androstane receptor (CAR;NR1I3) and pregnane X receptor (PXR;NR1I2) have been regarded as master regulators of drug disposition and detoxification mechanisms. They regulate the metabolism and transport of endogenous mediators and xenobiotics in organs including the liver, intestine and ...
Pablo Torres‐Vergara   +5 more
openaire   +2 more sources

The pregnane X receptor in tuberculosis therapeutics [PDF]

open access: yesExpert Opinion on Drug Metabolism & Toxicology, 2015
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
openaire   +2 more sources

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