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Interplay of the Organic Cation Transporters OCT1 and OCT2 with the Apically Localized Export Protein MATE1 for the Polarized Transport of Trospium

Molecular Pharmaceutics, 2019
The anticholinergic drug trospium is secreted into urine and, to a smaller extent, into bile. Chemically, it is an organic cation, and it is a substrate of the uptake transporters OCT1 and OCT2 as well as for the export proteins MATE1 and MATE2-K as determined in uptake studies using HEK293 cells.
Birgit Deutsch   +4 more
openaire   +2 more sources

Sex Differences in the mRNA, Protein, and Functional Expression of Organic Anion Transporter (Oat) 1, Oat3, and Organic Cation Transporter (Oct) 2 in Rabbit Renal Proximal Tubules

The Journal of Pharmacology and Experimental Therapeutics, 2006
Sex differences in transport of the organic anion (OA) substrate p-aminohippurate (PAH) and the organic cation (OC) substrate tetraethylammonium (TEA) have been recognized for some time. In the rat kidney, androgens up-regulate and estrogens down-regulate PAH and TEA transport, which correlate with similar changes in mRNA and protein expression for the
Carlotta E, Groves   +3 more
openaire   +2 more sources

Human Organic Cation Transporter 1 Protein Levels of Granulocytes Can Optimize Imatinib Therapy in Patients with Chronic Myeloid Leukemia

Acta Haematologica, 2014
The human organic cation transporter 1 (hOCT1) is the major active influx protein responsible for the transport of imatinib mesylate (IM) into cells. Previous studies have used <sup>14</sup>C-labeled IM to demonstrate a link between chronic myeloid leukemia (CML) molecular response and hOCT1 activity.
Chun, Cao   +5 more
openaire   +2 more sources

Mutation in an adaptor protein PDZK1 affects transport activity of organic cation transporter OCTNs and oligopeptide transporter PEPT2.

Drug metabolism and pharmacokinetics, 2007
Genetic polymorphisms in xenobiotic transporters have recently been clarified to be associated with change in drug distribution and disposition. To expand on recent identification of direct interaction and functional regulation of several transporters by a PDZ (PSD95, Dlg and ZO1) domain containing protein PDZK1, the effect of mutation in PDZK1 on ...
Tomoko, Sugiura   +3 more
openaire   +1 more source

Inhibition of gene expression of heart fatty acid binding protein and organic cation/carnitine transporter in doxorubicin cardiomyopathic rat model

European Journal of Pharmacology, 2010
This study examined whether doxorubicin therapy alters the expression of heart fatty acid binding protein (H-FABP) and organic cation/carnitine transporter (OCTN2) genes in cardiac tissues, and if so, whether these alterations contributes to doxorubicin-induced cardiotoxicity.
Mohamed M, Sayed-Ahmed   +4 more
openaire   +2 more sources

Citrus fruit‐derived flavonoid naringenin and the expression of hepatic organic cation transporter 1 protein in diabetic rats treated with metformin

Basic & Clinical Pharmacology & Toxicology, 2020
AbstractNaringenin possesses many pharmacological effects and may modulate metformin disposition. The purpose of this study was to evaluate the role of naringenin on hepatic expression of organic cation transporter 1 (OCT1) protein and its associated effects on metformin‐associated hyperlactataemia in diabetes.
Edith P, Mato Mofo   +2 more
openaire   +2 more sources

Wide variety of locations for rodent MATE1, a transporter protein that mediates the final excretion step for toxic organic cations

American Journal of Physiology-Cell Physiology, 2006
MATE1 was the first mammalian example of the multidrug and toxin extrusion (MATE) protein family to be identified. Human MATE1 (hMATE1) is predominantly expressed and localized to the luminal membranes of the urinary tubules and bile canaliculi and mediates H+-coupled electroneutral excretion of toxic organic cations (OCs) into urine and bile (Otsuka ...
Miki, Hiasa   +3 more
openaire   +2 more sources

An integrative approach to cisplatin chronic toxicities in mice reveals importance of organic cation-transporter-dependent protein networks for renoprotection

Archives of Toxicology, 2019
Cisplatin (CDDP) is one of the most important chemotherapeutic drugs in modern oncology. However, its use is limited by severe toxicities, which impair life quality after cancer. Here, we investigated the role of organic cation transporters (OCT) in mediating toxicities associated with chronic (twice the week for 4 weeks) low-dose (4 mg/kg body weight)
Anna Hucke   +24 more
openaire   +3 more sources

Role of organic cation transporter OCT2 and multidrug and toxin extrusion proteins MATE1 and MATE2-K for transport and drug interactions of the antiviral lamivudine

Biochemical Pharmacology, 2013
The antiviral lamivudine is cleared predominantly by the kidney with a relevant contribution of renal tubular secretion. It is not clear which drug transporters mediate lamivudine renal secretion. Our aim was to investigate lamivudine as substrate of the renal drug transporters organic cation transporter 2 (OCT2) and multidrug and toxin extrusion ...
Fabian, Müller   +4 more
openaire   +2 more sources

Regulation by protein kinase C of the contraluminal transport system for organic cations in rabbit kidney S2 proximal tubules.

The Journal of Pharmacology and Experimental Therapeutics, 1994
In the present study the effects of structurally different stimulators of protein kinase C (PKC) (phorbolesters and oleylacetylglycerol) as well as of staurosporine, a specific inhibitor of PKC activity, on the uptake of tetraethylammonium (TEA), a maker of the renal cation transport system, was investigated on isolated S2 segments of rabbit kidney ...
H, Hohage   +3 more
openaire   +2 more sources

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