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Studies on Functional Sites of Organic Cation/Carnitine Transporter OCTN2 (SLC22A5) Using a Ser467Cys Mutant Protein

The Journal of Pharmacology and Experimental Therapeutics, 2002
The organic cation/carnitine transporter OCTN2 mediates transport of carnitine and organic cations in Na(+)-dependent and Na(+)-independent manners, respectively. However, the mechanism of molecular recognition of different substrates has not been clarified yet. We previously found a single amino acid change in OCTN2, Ser467Cys (S467C), in the Japanese
Rikiya, Ohashi   +6 more
openaire   +2 more sources

PDZ Adaptor Protein PDZK2 Stimulates Transport Activity of Organic Cation/Carnitine Transporter OCTN2 by Modulating Cell Surface Expression

Drug Metabolism and Disposition, 2006
A part of the organic cation transporter families (OCT3, OCTN1, and OCTN2) has recently been identified to physically interact with PDZ (PSD95, Dlg, and ZO1) domain-containing proteins, although the physiological relevance of such interaction has not yet been fully examined.
Chizuru, Watanabe   +6 more
openaire   +2 more sources

Renal vectorial transport of berberine mediated by organic cation transporter 2 (OCT2) and multidrug and toxin extrusion proteins 1 (MATE1) in rats

Biopharmaceutics & Drug Disposition, 2017
AbstractBerberine, a well‐known plant alkaloid derived from Rhizoma coptidis, has potential applications as a therapeutic drug for diabetic nephropathy. However, the transporter‐mediated renal transport of berberine remains largely unclear. This study aimed to investigate the renal transport mechanism of berberine using transfected cells, kidney slices
Rong Shi   +7 more
openaire   +2 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

Protein kinase inhibition differentially regulates organic cation transport.

Canadian journal of physiology and pharmacology, 2010
Previous studies showed that amantadine transport increased while tetraethylammonium (TEA) transport decreased in kidney tissue from diabetic rats. Changes in transport activity were reversed by exogenous insulin. We hypothesized that this difference in transport regulation is due to differential regulation of different transport systems.
Alexander M, Gerlyand, Daniel S, Sitar
openaire   +1 more source

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

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

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

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

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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