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]
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]
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
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]
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
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
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]
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]
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]
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

