Results 41 to 50 of about 5,156 (193)

Regulation of CYP3A genes by glucocorticoids in human lung cells [v1; ref status: indexed, http://f1000r.es/1f9]

open access: yesF1000Research, 2013
Inhaled glucocorticoids are the first-line treatment for patients with persistent asthma.  However, approximately thirty percent of patients exhibit glucocorticoid insensitivity, which may involve excess metabolic clearance of the glucocorticoids by ...
Jessica K Roberts   +5 more
doaj   +1 more source

β-catenin signaling, the constitutive androstane receptor and their mutual interactions. [PDF]

open access: yesArch Toxicol, 2020
AbstractAberrant signaling through β-catenin is an important determinant of tumorigenesis in rodents as well as in humans. In mice, xenobiotic activators of the constitutive androstane receptor (CAR), a chemo-sensing nuclear receptor, promote liver tumor growth by means of a non-genotoxic mechanism and, under certain conditions, select for ...
Braeuning A, Pavek P.
europepmc   +4 more sources

Alternatively spliced isoforms of the human constitutive androstane receptor [PDF]

open access: yesNucleic Acids Research, 2003
The nuclear receptor CAR (NR1I3) regulates transcription of genes encoding xenobiotic- and steroid-metabolizing enzymes. Regulatory processes that are mediated by CAR are modulated by a structurally diverse array of chemicals including common pharmaceutical and environmental agents.
Scott S, Auerbach   +5 more
openaire   +2 more sources

A brief history of the discovery of PXR and CAR as xenobiotic receptors

open access: yesActa Pharmaceutica Sinica B, 2016
The nuclear receptors pregnane X receptor (PXR) and constitutive androstane receptor (CAR) were cloned and/or established as xenobiotic receptors in 1998.
Jiong Yan, Wen Xie
doaj   +1 more source

Dual action of oestrogens on the mouse constitutive androstane receptor [PDF]

open access: yesBiochemical Journal, 2003
mCAR (mouse constitutive androstane receptor; NR1I3) controls the expression of cytochrome P450 as well as other enzymes involved in drug and steroid metabolism. The high basal activity of mCAR can be modulated by inhibitory steroids related to androstenol and by activating xenobiotic chemicals such as 1,4-bis-[2-(3,5-dichloropyridyloxy)]benzene and ...
Janne, Mäkinen   +7 more
openaire   +2 more sources

CD-MPR: Quo Vadis? [PDF]

open access: yes, 2003
Lysosomes are membrane-bound organelles that serve in the degradation of many extracellular and intracellular macromolecules. Lysosomal biogenesis depends on the delivery of newly synthesized lysosomal hydrolases. This process requires the acquisition
Stöckli, Jacqueline
core   +1 more source

Stereoselective Biotransformation: Transfer of Learning to Advance Drug Metabolism and Biocatalysis

open access: yesAngewandte Chemie, Volume 138, Issue 25, 15 June 2026.
Understanding stereoselective biotransformations has implications for predicting drug disposition and response and may also inspire novel biocatalytic and biomimetic strategies to address challenges in metabolite and API synthesis. ABSTRACT Chirality is an important determinant of drug action, as enantiomers can exhibit markedly different ...
Grace A. Okunlola, Godwin A. Aleku
wiley   +2 more sources

Deciphering the roles of the constitutive androstane receptor in energy metabolism [PDF]

open access: yesActa Pharmacologica Sinica, 2014
The constitutive androstane receptor (CAR) is initially defined as a xenobiotic nuclear receptor that protects the liver from injury. Detoxification of damaging chemicals is achieved by CAR-mediated induction of drug-metabolizing enzymes and transporters.
Jiong, Yan   +3 more
openaire   +2 more sources

Regulation of hepatic heme synthesis by drugs, bile acids and nutrition : a transcriptional network regulating [delta]-aminolevulinic acid synthase 1 (ALAS1) [PDF]

open access: yes, 2008
ALAS1 is the rate limiting enzyme of heme synthesis. It is highly inducible in liver in cases of increased heme demand, such as drug metabolism or in inducible hepatic porphyrias.
Peyer, Anne-Kathrin
core   +1 more source

Dietary Flavonoids Activate the Constitutive Androstane Receptor (CAR) [PDF]

open access: yesJournal of Agricultural and Food Chemistry, 2010
The constitutive androstane receptor (CAR) is known as a xeno-sensor that regulates genes involved in xenobiotic excretion and energy metabolism. This study tested a variety of polyphenols for their ability to modulate CAR activity. HepG2 cells were transfected with a CAR expression plasmid and a reporter plasmid containing the human CYP2B6 regulatory ...
Ruiquing, Yao   +10 more
openaire   +2 more sources

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