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Rat Organic Cation Transporter 1 Contains Three Binding Sites for Substrate 1-Methyl-4-phenylpyridinium per Monomer.

Keller T, Gorboulev V, Mueller T, Dotsch V, Bernhard F, Koepsell H.

Mol Pharmacol. 2018 Nov 8. pii: mol.118.113498. doi: 10.1124/mol.118.113498. [Epub ahead of print]


Assay Conditions Influence Affinities of Rat Organic Cation Transporter 1: Analysis of Mutagenesis in the Modeled Outward-Facing Cleft by Measuring Effects of Substrates and Inhibitors on Initial Uptake.

Gorboulev V, Rehman S, Albert CM, Roth U, Meyer MJ, Tzvetkov MV, Mueller TD, Koepsell H.

Mol Pharmacol. 2018 Apr;93(4):402-415. doi: 10.1124/mol.117.110767. Epub 2018 Jan 16.


Protein RS1 (RSC1A1) Downregulates the Exocytotic Pathway of Glucose Transporter SGLT1 at Low Intracellular Glucose via Inhibition of Ornithine Decarboxylase.

Chintalapati C, Keller T, Mueller TD, Gorboulev V, Schäfer N, Zilkowski I, Veyhl-Wichmann M, Geiger D, Groll J, Koepsell H.

Mol Pharmacol. 2016 Nov;90(5):508-521. Epub 2016 Aug 23.


Phosphorylation of RS1 (RSC1A1) Steers Inhibition of Different Exocytotic Pathways for Glucose Transporter SGLT1 and Nucleoside Transporter CNT1, and an RS1-Derived Peptide Inhibits Glucose Absorption.

Veyhl-Wichmann M, Friedrich A, Vernaleken A, Singh S, Kipp H, Gorboulev V, Keller T, Chintalapati C, Pipkorn R, Pastor-Anglada M, Groll J, Koepsell H.

Mol Pharmacol. 2016 Jan;89(1):118-32. doi: 10.1124/mol.115.101162. Epub 2015 Oct 13.


Central nervous system infiltrates are characterized by features of ongoing B cell-related immune activity in MP4-induced experimental autoimmune encephalomyelitis.

Batoulis H, Wunsch M, Birkenheier J, Rottlaender A, Gorboulev V, Kuerten S.

Clin Immunol. 2015 May;158(1):47-58. doi: 10.1016/j.clim.2015.03.009. Epub 2015 Mar 18.


Nucleoside transporters and human organic cation transporter 1 determine the cellular handling of DNA-methyltransferase inhibitors.

Arimany-Nardi C, Errasti-Murugarren E, Minuesa G, Martinez-Picado J, Gorboulev V, Koepsell H, Pastor-Anglada M.

Br J Pharmacol. 2014 Aug;171(16):3868-80. doi: 10.1111/bph.12748.


Substrate- and cell contact-dependent inhibitor affinity of human organic cation transporter 2: studies with two classical organic cation substrates and the novel substrate cd2+.

Thévenod F, Ciarimboli G, Leistner M, Wolff NA, Lee WK, Schatz I, Keller T, Al-Monajjed R, Gorboulev V, Koepsell H.

Mol Pharm. 2013 Aug 5;10(8):3045-56. doi: 10.1021/mp400113d. Epub 2013 Jun 24.


A substrate binding hinge domain is critical for transport-related structural changes of organic cation transporter 1.

Egenberger B, Gorboulev V, Keller T, Gorbunov D, Gottlieb N, Geiger D, Mueller TD, Koepsell H.

J Biol Chem. 2012 Sep 7;287(37):31561-73. doi: 10.1074/jbc.M112.388793. Epub 2012 Jul 18.


Na(+)-D-glucose cotransporter SGLT1 is pivotal for intestinal glucose absorption and glucose-dependent incretin secretion.

Gorboulev V, Schürmann A, Vallon V, Kipp H, Jaschke A, Klessen D, Friedrich A, Scherneck S, Rieg T, Cunard R, Veyhl-Wichmann M, Srinivasan A, Balen D, Breljak D, Rexhepaj R, Parker HE, Gribble FM, Reimann F, Lang F, Wiese S, Sabolic I, Sendtner M, Koepsell H.

Diabetes. 2012 Jan;61(1):187-96. doi: 10.2337/db11-1029. Epub 2011 Nov 28.


The large extracellular loop of organic cation transporter 1 influences substrate affinity and is pivotal for oligomerization.

Keller T, Egenberger B, Gorboulev V, Bernhard F, Uzelac Z, Gorbunov D, Wirth C, Koppatz S, Dötsch V, Hunte C, Sitte HH, Koepsell H.

J Biol Chem. 2011 Oct 28;286(43):37874-86. doi: 10.1074/jbc.M111.289330. Epub 2011 Sep 6.


Novel shuttling domain in a regulator (RSC1A1) of transporter SGLT1 steers cell cycle-dependent nuclear location.

Filatova A, Leyerer M, Gorboulev V, Chintalapati C, Reinders Y, Müller TD, Srinivasan A, Hübner S, Koepsell H.

Traffic. 2009 Nov;10(11):1599-618. doi: 10.1111/j.1600-0854.2009.00982.x. Epub 2009 Sep 2.


Five amino acids in the innermost cavity of the substrate binding cleft of organic cation transporter 1 interact with extracellular and intracellular corticosterone.

Volk C, Gorboulev V, Kotzsch A, Müller TD, Koepsell H.

Mol Pharmacol. 2009 Aug;76(2):275-89. doi: 10.1124/mol.109.054783. Epub 2009 May 12.


Charge-to-substrate ratio during organic cation uptake by rat OCT2 is voltage dependent and altered by exchange of glutamate 448 with glutamine.

Schmitt BM, Gorbunov D, Schlachtbauer P, Egenberger B, Gorboulev V, Wischmeyer E, Müller T, Koepsell H.

Am J Physiol Renal Physiol. 2009 Apr;296(4):F709-22. doi: 10.1152/ajprenal.90323.2008. Epub 2009 Feb 11.


Transport of lamivudine [(-)-beta-L-2',3'-dideoxy-3'-thiacytidine] and high-affinity interaction of nucleoside reverse transcriptase inhibitors with human organic cation transporters 1, 2, and 3.

Minuesa G, Volk C, Molina-Arcas M, Gorboulev V, Erkizia I, Arndt P, Clotet B, Pastor-Anglada M, Koepsell H, Martinez-Picado J.

J Pharmacol Exp Ther. 2009 Apr;329(1):252-61. doi: 10.1124/jpet.108.146225. Epub 2009 Jan 13. Erratum in: J Pharmacol Exp Ther. 2009 Jun;329(3):1187.


Cell free expression and functional reconstitution of eukaryotic drug transporters.

Keller T, Schwarz D, Bernhard F, Dötsch V, Hunte C, Gorboulev V, Koepsell H.

Biochemistry. 2008 Apr 15;47(15):4552-64. doi: 10.1021/bi800060w. Epub 2008 Mar 25.


High-affinity cation binding to organic cation transporter 1 induces movement of helix 11 and blocks transport after mutations in a modeled interaction domain between two helices.

Gorbunov D, Gorboulev V, Shatskaya N, Mueller T, Bamberg E, Friedrich T, Koepsell H.

Mol Pharmacol. 2008 Jan;73(1):50-61. Epub 2007 Oct 16.


Tripeptides of RS1 (RSC1A1) inhibit a monosaccharide-dependent exocytotic pathway of Na+-D-glucose cotransporter SGLT1 with high affinity.

Vernaleken A, Veyhl M, Gorboulev V, Kottra G, Palm D, Burckhardt BC, Burckhardt G, Pipkorn R, Beier N, van Amsterdam C, Koepsell H.

J Biol Chem. 2007 Sep 28;282(39):28501-13. Epub 2007 Aug 8.


Identification of cysteines in rat organic cation transporters rOCT1 (C322, C451) and rOCT2 (C451) critical for transport activity and substrate affinity.

Sturm A, Gorboulev V, Gorbunov D, Keller T, Volk C, Schmitt BM, Schlachtbauer P, Ciarimboli G, Koepsell H.

Am J Physiol Renal Physiol. 2007 Sep;293(3):F767-79. Epub 2007 Jun 13.


Transporter regulator RS1 (RSC1A1) coats the trans-Golgi network and migrates into the nucleus.

Kroiss M, Leyerer M, Gorboulev V, Kühlkamp T, Kipp H, Koepsell H.

Am J Physiol Renal Physiol. 2006 Dec;291(6):F1201-12. Epub 2006 Jun 20.


RS1 (RSC1A1) regulates the exocytotic pathway of Na+-D-glucose cotransporter SGLT1.

Veyhl M, Keller T, Gorboulev V, Vernaleken A, Koepsell H.

Am J Physiol Renal Physiol. 2006 Dec;291(6):F1213-23. Epub 2006 Jun 20.


Characterization of regulatory mechanisms and states of human organic cation transporter 2.

Biermann J, Lang D, Gorboulev V, Koepsell H, Sindic A, Schröter R, Zvirbliene A, Pavenstädt H, Schlatter E, Ciarimboli G.

Am J Physiol Cell Physiol. 2006 Jun;290(6):C1521-31. Epub 2006 Jan 4.


Rat renal glucose transporter SGLT1 exhibits zonal distribution and androgen-dependent gender differences.

Sabolić I, Skarica M, Gorboulev V, Ljubojević M, Balen D, Herak-Kramberger CM, Koepsell H.

Am J Physiol Renal Physiol. 2006 Apr;290(4):F913-26. Epub 2005 Oct 4.


Purification and functional reconstitution of the rat organic cation transporter OCT1.

Keller T, Elfeber M, Gorboulev V, Reiländer H, Koepsell H.

Biochemistry. 2005 Sep 13;44(36):12253-63.


Individual PKC-phosphorylation sites in organic cation transporter 1 determine substrate selectivity and transport regulation.

Ciarimboli G, Koepsell H, Iordanova M, Gorboulev V, Dürner B, Lang D, Edemir B, Schröter R, Van Le T, Schlatter E.

J Am Soc Nephrol. 2005 Jun;16(6):1562-70. Epub 2005 Apr 13.


Amino acids critical for substrate affinity of rat organic cation transporter 1 line the substrate binding region in a model derived from the tertiary structure of lactose permease.

Popp C, Gorboulev V, Müller TD, Gorbunov D, Shatskaya N, Koepsell H.

Mol Pharmacol. 2005 May;67(5):1600-11. Epub 2005 Jan 20.


Mice without the regulator gene Rsc1A1 exhibit increased Na+-D-glucose cotransport in small intestine and develop obesity.

Osswald C, Baumgarten K, Stümpel F, Gorboulev V, Akimjanova M, Knobeloch KP, Horak I, Kluge R, Joost HG, Koepsell H.

Mol Cell Biol. 2005 Jan;25(1):78-87.


Regulation of the human organic cation transporter hOCT1.

Ciarimboli G, Struwe K, Arndt P, Gorboulev V, Koepsell H, Schlatter E, Hirsch JR.

J Cell Physiol. 2004 Dec;201(3):420-8.


Na(+)-D-glucose cotransporter in muscle capillaries increases glucose permeability.

Elfeber K, Stümpel F, Gorboulev V, Mattig S, Deussen A, Kaissling B, Koepsell H.

Biochem Biophys Res Commun. 2004 Feb 6;314(2):301-5.


Downregulation of the Na(+)- D-glucose cotransporter SGLT1 by protein RS1 (RSC1A1) is dependent on dynamin and protein kinase C.

Veyhl M, Wagner CA, Gorboulev V, Schmitt BM, Lang F, Koepsell H.

J Membr Biol. 2003 Nov 1;196(1):71-81.


Different affinities of inhibitors to the outwardly and inwardly directed substrate binding site of organic cation transporter 2.

Volk C, Gorboulev V, Budiman T, Nagel G, Koepsell H.

Mol Pharmacol. 2003 Nov;64(5):1037-47.


A glucose sensor hiding in a family of transporters.

Diez-Sampedro A, Hirayama BA, Osswald C, Gorboulev V, Baumgarten K, Volk C, Wright EM, Koepsell H.

Proc Natl Acad Sci U S A. 2003 Sep 30;100(20):11753-8. Epub 2003 Sep 16.


Organic cation transporters.

Koepsell H, Schmitt BM, Gorboulev V.

Rev Physiol Biochem Pharmacol. 2003;150:36-90. Epub 2003 Jun 25. Review.


Organic cation transporter capable of transporting serotonin is up-regulated in serotonin transporter-deficient mice.

Schmitt A, Mössner R, Gossmann A, Fischer IG, Gorboulev V, Murphy DL, Koepsell H, Lesch KP.

J Neurosci Res. 2003 Mar 1;71(5):701-9.


Identification of genetic variations of the human organic cation transporter hOCT1 and their functional consequences.

Kerb R, Brinkmann U, Chatskaia N, Gorbunov D, Gorboulev V, Mornhinweg E, Keil A, Eichelbaum M, Koepsell H.

Pharmacogenetics. 2002 Nov;12(8):591-5.


The cation transporters rOCT1 and rOCT2 interact with bicarbonate but play only a minor role for amantadine uptake into rat renal proximal tubules.

Goralski KB, Lou G, Prowse MT, Gorboulev V, Volk C, Koepsell H, Sitar DS.

J Pharmacol Exp Ther. 2002 Dec;303(3):959-68.


Regulation of human organic cation transporter hOCT2 by PKA, PI3K, and calmodulin-dependent kinases.

Cetinkaya I, Ciarimboli G, Yalçinkaya G, Mehrens T, Velic A, Hirsch JR, Gorboulev V, Koepsell H, Schlatter E.

Am J Physiol Renal Physiol. 2003 Feb;284(2):F293-302. Epub 2002 Oct 15.


The plasma membrane-associated protein RS1 decreases transcription of the transporter SGLT1 in confluent LLC-PK1 cells.

Korn T, Kühlkamp T, Track C, Schatz I, Baumgarten K, Gorboulev V, Koepsell H.

J Biol Chem. 2001 Nov 30;276(48):45330-40. Epub 2001 Sep 18.


Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1.

Arndt P, Volk C, Gorboulev V, Budiman T, Popp C, Ulzheimer-Teuber I, Akhoundova A, Koppatz S, Bamberg E, Nagel G, Koepsell H.

Am J Physiol Renal Physiol. 2001 Sep;281(3):F454-68.


Structure and Function of Renal Organic Cation Transporters.

Koepsell H, Busch A, Gorboulev V, Arndt P.

News Physiol Sci. 1998 Feb;13:11-16.


Polyspecific cation transporters in the proximal tubule.

Koepsell H, Gorboulev V, Karbach U, Arndt P.

Nephrol Dial Transplant. 2000;15 Suppl 6:3-4. Review. No abstract available.


Localization of organic cation transporters OCT1 and OCT2 in rat kidney.

Karbach U, Kricke J, Meyer-Wentrup F, Gorboulev V, Volk C, Loffing-Cueni D, Kaissling B, Bachmann S, Koepsell H.

Am J Physiol Renal Physiol. 2000 Oct;279(4):F679-87.


The affinity of the organic cation transporter rOCT1 is increased by protein kinase C-dependent phosphorylation.

Mehrens T, Lelleck S, Cetinkaya I, Knollmann M, Hohage H, Gorboulev V, Bokník P, Koepsell H, Schlatter E.

J Am Soc Nephrol. 2000 Jul;11(7):1216-24.


Selectivity of the polyspecific cation transporter rOCT1 is changed by mutation of aspartate 475 to glutamate.

Gorboulev V, Volk C, Arndt P, Akhoundova A, Koepsell H.

Mol Pharmacol. 1999 Dec;56(6):1254-61.


Molecular pharmacology of organic cation transporters in kidney.

Koepsell H, Gorboulev V, Arndt P.

J Membr Biol. 1999 Jan 15;167(2):103-17. Review. No abstract available.


Membrane localization of the electrogenic cation transporter rOCT1 in rat liver.

Meyer-Wentrup F, Karbach U, Gorboulev V, Arndt P, Koepsell H.

Biochem Biophys Res Commun. 1998 Jul 30;248(3):673-8.


Human neurons express the polyspecific cation transporter hOCT2, which translocates monoamine neurotransmitters, amantadine, and memantine.

Busch AE, Karbach U, Miska D, Gorboulev V, Akhoundova A, Volk C, Arndt P, Ulzheimer JC, Sonders MS, Baumann C, Waldegger S, Lang F, Koepsell H.

Mol Pharmacol. 1998 Aug;54(2):342-52.


Transport of the new chemotherapeutic agent beta-D-glucosylisophosphoramide mustard (D-19575) into tumor cells is mediated by the Na+-D-glucose cotransporter SAAT1.

Veyhl M, Wagner K, Volk C, Gorboulev V, Baumgarten K, Weber WM, Schaper M, Bertram B, Wiessler M, Koepsell H.

Proc Natl Acad Sci U S A. 1998 Mar 17;95(6):2914-9.


Cloning and characterization of two human polyspecific organic cation transporters.

Gorboulev V, Ulzheimer JC, Akhoundova A, Ulzheimer-Teuber I, Karbach U, Quester S, Baumann C, Lang F, Busch AE, Koepsell H.

DNA Cell Biol. 1997 Jul;16(7):871-81.


The two human organic cation transporter genes SLC22A1 and SLC22A2 are located on chromosome 6q26.

Koehler MR, Wissinger B, Gorboulev V, Koepsell H, Schmid M.

Cytogenet Cell Genet. 1997;79(3-4):198-200.


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