Regulation of the human organic cation transporter hOCT1

Journal of Cellular Physiology
Giuliano CiarimboliJochen R Hirsch

Abstract

The human organic cation transporter type 1 (hOCT1) is an important transport system for small organic cations in the liver. Organic cation transporters are regulated by different signaling pathways, but the regulation of hOCT1 has not yet been studied. In this work, we have for the first time investigated the regulation of hOCT1. hOCT1 was expressed in Chinese hamster ovary cells (CHO-hOCT1) and in human embryonic kidney cells (HEK293-hOCT1). Its activity was monitored using microfluorimetry with the fluorescent organic cation 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP(+)) as substrate. hOCT1 expressed in CHO-cells was inhibited by protein kinase A (PKA) activation (1 microM forskolin, -58 +/- 6%, n = 12), calmodulin inhibition (0.1 microM calmidazolium, -68 +/- 3%, n = 6; 10 microM ophiobolin A, -48 +/- 10%, n = 7), calmodulin-dependent kinase II inhibition (1 microM KN62, -78 +/- 4%, n = 12), and inhibition of p56(lck) tyrosine kinase (10 microM aminogenistein, -35 +/- 7%, n = 12). The apparent affinities for TEA(+) were lower in CHO-hOCT1 than in HEK293-hOCT1, while those for TPA(+) and quinine were almost identical; the rank order of EC(50) values (TPA(+) > quinine > TEA(+)) was independent of the expression syste...Continue Reading

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Citations

Feb 3, 2005·Pflügers Archiv : European journal of physiology·Giuliano Ciarimboli, Eberhard Schlatter
Jan 28, 2010·Pharmacological Reviews·Curtis D Klaassen, Lauren M Aleksunes
Nov 16, 2013·Pflügers Archiv : European journal of physiology·Eberhard SchlatterGiuliano Ciarimboli
May 10, 2011·Cellular and Molecular Life Sciences : CMLS·A GrabnerG Ciarimboli
Jan 31, 2015·Expert Opinion on Drug Metabolism & Toxicology·Candido G Da SilvaGodefridus J Peters
Jan 19, 2011·Expert Opinion on Drug Metabolism & Toxicology·Giuliano Ciarimboli
Aug 1, 2008·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·G Ciarimboli
Nov 30, 2005·The American Journal of Pathology·Giuliano CiarimboliEberhard Schlatter
Nov 6, 2007·Biochemical Pharmacology·Erik Rytting, Kenneth L Audus
Dec 17, 2014·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Lydia AschauerPaul Jennings
Jul 20, 2007·Fundamental & Clinical Pharmacology·Vera Dias, Vera Ribeiro
Jun 29, 2004·Trends in Pharmacological Sciences·Hermann Koepsell
Jun 3, 2014·Journal of Experimental & Clinical Cancer Research : CR·Ruijin ShaoHåkan Billig
Apr 5, 2017·International Journal of Molecular Sciences·Abdullah MayatiOlivier Fardel
Apr 15, 2005·Journal of the American Society of Nephrology : JASN·Giuliano CiarimboliEberhard Schlatter
Oct 1, 2005·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Bruce KwokShinya Ito
Jan 6, 2006·American Journal of Physiology. Cell Physiology·Jürgen BiermannGiuliano Ciarimboli
Jul 12, 2005·The Journal of Pharmacology and Experimental Therapeutics·Harunobu TaharaYuichi Sugiyama
Jan 27, 2006·The Journal of Pharmacology and Experimental Therapeutics·Michael SaborowskiJyrki J Eloranta
Dec 20, 2019·Pharmacological Reviews·Hermann Koepsell
Jul 28, 2020·International Journal of Molecular Sciences·Marta KantauskaitėGiuliano Ciarimboli
Mar 19, 2021·Frontiers in Pharmacology·Giuliano Ciarimboli
Sep 16, 2008·Journal of Medicinal Chemistry·Gustav AhlinPer Artursson
May 1, 2021·International Journal of Molecular Sciences·Anne-Margarethe EngeStefanie Hessel-Pras
Jun 15, 2021·Frontiers in Cell and Developmental Biology·Sandra SchornGiuliano Ciarimboli

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