The pregnane X receptor down‐regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for (“squelching”) SRC‐1 coactivator

L Hyrsova, T Smutny, A Carazo… - British Journal of …, 2016 - Wiley Online Library
Background and Purpose The organic cation transporter 1 (OCT1) transports cationic drugs
into hepatocytes. The high hepatic expression of OCT1 is controlled by the HNF4α and USF …

Expression of organic cation transporter 1 (OCT1): unique patterns of indirect regulation by nuclear receptors and hepatospecific gene regulation

L Hyrsova, T Smutny, F Trejtnar… - Drug metabolism reviews, 2016 - Taylor & Francis
The organic cation transporter 1 (OCT1) is the dominant carrier of organic cationic drugs and
some positively charged endogenous compounds into hepatocytes. OCT1 has unique …

Effect of pregnane X receptor ligand on pharmacokinetics of substrates of organic cation transporter Oct1 in rats

T Maeda, M Oyabu, T Yotsumoto, R Higashi… - Drug metabolism and …, 2007 - ASPET
Because rat organic cation transporter 1 (Oct1, SLC22a1) is expressed mainly in the liver
and mediates drug transport, its activity may determine the hepatic handling of cationic …

Identification of pregnane X receptor binding sites in the regulatory regions of genes involved in bile acid homeostasis

C Frank, H Makkonen, TW Dunlop, M Matilainen… - Journal of molecular …, 2005 - Elsevier
The nuclear receptor pregnane X receptor (PXR) acts as a sensor for a broad variety of
natural and synthetic lipophilic compounds, such as bile acids and rifampicin, and regulates …

Ligand-activated pregnane X receptor interferes with HNF-4 signaling by targeting a common coactivator PGC-1α: functional implications in hepatic cholesterol and …

S Bhalla, C Ozalp, S Fang, L Xiang… - Journal of Biological …, 2004 - ASBMB
Previous studies show that feedback inhibition of bile acid production by bile acids is
mediated by multiple mechanisms, including activation of pregnane X receptor (PXR) …

Pharmacokinetics of organic cation transporter 1 (OCT1) substrates in Oct1/2 knockout mice and species difference in hepatic OCT1-mediated uptake

BL Morse, A Kolur, LR Hudson, AT Hogan… - Drug Metabolism and …, 2020 - ASPET
Organic cation transporter 1 (OCT1) plays a role in hepatic uptake of drugs, affecting in vivo
exposure, distinguished primarily through pharmacogenetics of the SLC22A1 gene. The role …

SLC13A5 is a novel transcriptional target of the pregnane X receptor and sensitizes drug-induced steatosis in human liver

L Li, H Li, B Garzel, H Yang, T Sueyoshi, Q Li… - Molecular …, 2015 - ASPET
The solute carrier family 13 member 5 (SLC13A5) is a sodium-coupled transporter that
mediates cellular uptake of citrate, which plays important roles in the synthesis of fatty acids …

Novel single nucleotide polymorphisms in the promoter and intron 1 of human pregnane X receptor/NR1I2 and their association with CYP3A4 expression

J Lamba, V Lamba, S Strom, R Venkataramanan… - Drug metabolism and …, 2008 - ASPET
The hypothesis was tested that sequence diversity in pregnane X receptor (PXR) cis-
regulatory regions is a significant determinant of variation in inducible and constitutive …

Induction of rat organic anion transporting polypeptide 2 by pregnenolone-16α-carbonitrile is via interaction with pregnane X receptor

GL Guo, J Staudinger, K Ogura, CD Klaassen - Molecular pharmacology, 2002 - ASPET
The rat organic anion transporting polypeptide 2 (oatp2; Slc21a5) is a liver transporter that
mediates the uptake of a variety of structurally diverse compounds, and has a high affinity for …

Regulation of basal core promoter activity of human organic cation transporter 1 (OCT1/SLC22A1)

M Kajiwara, T Terada, J Asaka, M Aoki… - American Journal …, 2008 - journals.physiology.org
Human organic cation transporter 1 (OCT1/SLC22A1) plays important roles in the hepatic
uptake of cationic drugs. The functional characteristics of this transporter have been well …