Results 141 to 150 of about 12,669 (162)

Pxr, car and drug metabolism

Nature Reviews Drug Discovery, 2002
Mechanisms that protect the body from a diverse array of harmful chemicals are also involved in drug metabolism, and can cause adverse drug-drug interactions. Two closely related orphan nuclear hormone receptors--the pregnane X receptor (PXR) and the constitutive androstane receptor (CAR)--have recently emerged as transcriptional regulators of ...
Timothy M, Willson, Steven A, Kliewer
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Unique Transcription Start Sites and Distinct Promoter Regions Differentiate the Pregnane X Receptor (PXR) Isoforms PXR 1 and PXR 2

Drug Metabolism and Disposition, 2008
The pregnane X receptor (PXR) is known as the xenosensing receptor responsible for coordinated regulation of metabolic genes in response to diverse xenobiotic challenges. In particular, the ability of the PXR to regulate CYP3A4, the enzyme capable of metabolizing more than 60% of all pharmaceuticals, defines its metabolic importance. Currently the list
Leslie M, Tompkins, Tim L, Sit, Andrew D, Wallace   +2 more
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PXR and CAR in energy metabolism

Trends in Endocrinology & Metabolism, 2009
The nuclear receptors pregnane X receptor (PXR, or NR1I2) and constitutive androstane receptor (CAR, or NR1I3) were originally identified as xenosensors that regulate the expression of Phase I and Phase II drug-metabolizing enzymes and transporters. Recent results suggest that PXR and CAR also have important endobiotic roles in energy metabolism by ...
Taira, Wada, Jie, Gao, Wen, Xie
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PXR mediates mifepristone-induced hepatomegaly in mice

Acta Pharmacologica Sinica, 2021
Mifepristone (Mif), an effective synthetic steroidal antiprogesterone drug, is widely used for medical abortion and pregnancy prevention. Due to its anti-glucocorticoid effect, high-dose Mif is also used to treat Cushing's syndrome. Mif was reported to active pregnane X receptor (PXR) in vitro and PXR can induce hepatomegaly via activation and ...
Xin-Peng, Yao, Ting-Ying, Jiao, Yi-Ming, Jiang, Shi-Cheng, Fan, Ying-Yuan, Zhao, Xiao, Yang, Yue, Gao, Fei, Li, Yan-Ying, Zhou, Pan-Pan, Chen, Min, Huang, Hui-Chang, Bi   +11 more
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CAR and PXR: Xenosensors of endocrine disrupters?

Chemico-Biological Interactions, 2005
The pregnane X-receptor (PXR) and the constitutive androstane receptor (CAR) are orphan nuclear receptors activated by a variety of ligands. Currently it remains uncertain whether these receptors have a high-affinity ligand or instead function as more generalized steroid/xenobiotic sensors. Both receptors are important regulators of several steroid and
Xiomara C, Kretschmer, William S, Baldwin   +1 more
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Genetic Variability of PXR in Saudi Arabians

Biochemical Genetics, 2013
Polymorphisms in the PXR gene play important roles in influencing the efficacy and toxicity of a large number of endogenous and exogenous substrates. Because of ethnic specificity, several studies have been directed toward the determination of PXR polymorphisms in various populations.
Mohammed S, Al-Dosari, Khalid M, Alkharfy, Amal M, Alghamdi, Abdullah M, Al-Mohizea, Fahad I, Al-Jenoobi, Saleh, Al-Muhsen, Rabih, Halwani, M Khalid, Parvez, M, Khalid Parvez   +8 more
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FXR and PXR

Journal of steroid biochemistry and molecular biology, 2012
Cholestatic liver disorders encompass hepatobiliary diseases of diverse etiologies characterized by the accumulation of bile acids, bilirubin and cholesterol as the result of impaired secretion of bile. Members of the nuclear receptor (NR) family of ligand-modulated transcription factors are implicated in the adaptive response to cholestasis.
Jonker, Johan W., Liddle, Christopher, Downes, Michael   +2 more
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Xenobiotic Receptors CAR and PXR

2010
The absorption, distribution, metabolism, and excretion (ADME) of chemicals are coordinately fulfilled by drug transporters as well as phase-I and phase-II drug-metabolizing enzymes. The two so-called “xenobiotic receptors”, namely constitutive active/androstane receptor (CAR, NR1I3) and pregnane X receptor (PXR, NR1I2), are predominantly expressed in ...
Curtis Klaassen, Hong Lu
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Regulation of Pregnane X Receptor (PXR) Function and UGT1A1 Gene Expression by Posttranslational Modification of PXR Protein

Drug Metabolism and Disposition, 2012
Human UDP-glucuronosyltransferase (UGT) 1A1 is a critical enzyme responsible for detoxification and metabolism of endogenous and exogenous lipophilic compounds such as bilirubin. The present study shows how cyclin-dependent kinase (CDK) inhibitor roscovitine stimulated the expression of UGT1A1 in HepG2 cells.
Junko, Sugatani, Takahiro, Uchida, Masatoshi, Kurosawa, Masahiko, Yamaguchi, Yasuhiro, Yamazaki, Akira, Ikari, Masao, Miwa   +6 more
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Irinotécan : UGT et PXR

2013
L’irinotecan a largement contribue aux importants progres realises ces quinze dernieres annees dans le traitement des cancers digestifs, et il occupe dorenavant une place majeure en cancerologie digestive. Developpe initialement dans le traitement du cancer colorectal avance pour lequel il est largement prescrit, l’irinotecan est egalement indique dans
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