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Renal Olfactory Receptor 1393 Contributes to the Progression of Type II Diabetes in a Diet-Induced Obesity Model.

Shepard BD, Koepsell H, Pluznick JL.

Am J Physiol Renal Physiol. 2018 Nov 28. doi: 10.1152/ajprenal.00069.2018. [Epub ahead of print]


SGLT2 inhibition and renal urate excretion: the role of luminal glucose, GLUT9 and URAT1.

Novikov A, Fu Y, Huang W, Freeman B, Patel R, van Ginkel C, Koepsell H, Busslinger M, Onishi A, Nespoux J, Vallon V.

Am J Physiol Renal Physiol. 2018 Nov 14. doi: 10.1152/ajprenal.00462.2018. [Epub ahead of print]


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]


A Modified Tripeptide Motif of RS1 (RSC1A1) Down-Regulates Exocytotic Pathways of Human Na+-d-glucose Cotransporters SGLT1, SGLT2, and Glucose Sensor SGLT3 in the Presence of Glucose.

Schäfer N, Rikkala PR, Veyhl-Wichmann M, Keller T, Jurowich CF, Geiger D, Koepsell H.

Mol Pharmacol. 2019 Jan;95(1):82-96. doi: 10.1124/mol.118.113514. Epub 2018 Oct 24.


Functional analysis of a triplet deletion in the gene encoding the sodium glucose transporter 3, a potential risk factor for ADHD.

Schäfer N, Friedrich M, Jørgensen ME, Kollert S, Koepsell H, Wischmeyer E, Lesch KP, Geiger D, Döring F.

PLoS One. 2018 Oct 4;13(10):e0205109. doi: 10.1371/journal.pone.0205109. eCollection 2018.


Loss of MYO5B Leads to Reductions in Na+ Absorption With Maintenance of CFTR-Dependent Cl- Secretion in Enterocytes.

Engevik AC, Kaji I, Engevik MA, Meyer AR, Weis VG, Goldstein A, Hess MW, Müller T, Koepsell H, Dudeja PK, Tyska M, Huber LA, Shub MD, Ameen N, Goldenring JR.

Gastroenterology. 2018 Dec;155(6):1883-1897.e10. doi: 10.1053/j.gastro.2018.08.025. Epub 2018 Aug 23.


Multiple binding sites in organic cation transporters require sophisticated procedures to identify interactions of novel drugs.

Koepsell H.

Biol Chem. 2018 Sep 11. pii: /j/bchm.ahead-of-print/hsz-2018-0191/hsz-2018-0191.xml. doi: 10.1515/hsz-2018-0191. [Epub ahead of print] Review.


Chronic Pressure Overload Induces Cardiac Hypertrophy and Fibrosis via Increases in SGLT1 and IL-18 Gene Expression in Mice.

Matsushita N, Ishida N, Ibi M, Saito M, Sanbe A, Shimojo H, Suzuki S, Koepsell H, Takeishi Y, Morino Y, Taira E, Sawa Y, Hirose M.

Int Heart J. 2018 Sep 26;59(5):1123-1133. doi: 10.1536/ihj.17-565. Epub 2018 Aug 11.


RS1 (Rsc1A1) deficiency limits cerebral SGLT1 expression and delays brain damage after experimental traumatic brain injury.

Sebastiani A, Greve F, Gölz C, Förster CY, Koepsell H, Thal SC.

J Neurochem. 2018 Oct;147(2):190-203. doi: 10.1111/jnc.14551. Epub 2018 Sep 20.


Altered pancreatic islet morphology and function in SGLT1 knockout mice on a glucose-deficient, fat-enriched diet.

Mühlemann M, Zdzieblo D, Friedrich A, Berger C, Otto C, Walles H, Koepsell H, Metzger M.

Mol Metab. 2018 Jul;13:67-76. doi: 10.1016/j.molmet.2018.05.011. Epub 2018 May 23.


Unmasking a sustained negative effect of SGLT2 inhibition on body fluid volume in the rat.

Masuda T, Watanabe Y, Fukuda K, Watanabe M, Onishi A, Ohara K, Imai T, Koepsell H, Muto S, Vallon V, Nagata D.

Am J Physiol Renal Physiol. 2018 Sep 1;315(3):F653-F664. doi: 10.1152/ajprenal.00143.2018. Epub 2018 May 23.


Organic anion transporter OAT3 enhances the glucosuric effect of the SGLT2 inhibitor empagliflozin.

Fu Y, Breljak D, Onishi A, Batz F, Patel R, Huang W, Song P, Freeman B, Mayoux E, Koepsell H, Anzai N, Nigam SK, Sabolic I, Vallon V.

Am J Physiol Renal Physiol. 2018 Aug 1;315(2):F386-F394. doi: 10.1152/ajprenal.00503.2017. Epub 2018 Feb 7.


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.


Loss of Endometrial Sodium Glucose Cotransporter SGLT1 is Detrimental to Embryo Survival and Fetal Growth in Pregnancy.

Salker MS, Singh Y, Zeng N, Chen H, Zhang S, Umbach AT, Fakhri H, Kohlhofer U, Quintanilla-Martinez L, Durairaj RRP, Barros FSV, Vrljicak P, Ott S, Brucker SY, Wallwiener D, Vrhovac Madunić I, Breljak D, Sabolić I, Koepsell H, Brosens JJ, Lang F.

Sci Rep. 2017 Oct 3;7(1):12612. doi: 10.1038/s41598-017-11674-3.


Expression profiling and immunolocalization of Na+-D-glucose-cotransporter 1 in mice employing knockout mice as specificity control indicate novel locations and differences between mice and rats.

Madunić IV, Breljak D, Karaica D, Koepsell H, Sabolić I.

Pflugers Arch. 2017 Dec;469(12):1545-1565. doi: 10.1007/s00424-017-2056-1. Epub 2017 Aug 26.


SGLT1 Deficiency Turns Listeria Infection into a Lethal Disease in Mice.

Sharma P, Khairnar V, Madunić IV, Singh Y, Pandyra A, Salker MS, Koepsell H, Sabolić I, Lang F, Lang PA, Lang KS.

Cell Physiol Biochem. 2017;42(4):1358-1365. doi: 10.1159/000479197. Epub 2017 Jul 14.


Sodium-glucose co-transporter (SGLT)2 and SGLT1 renal expression in patients with type 2 diabetes.

Solini A, Rossi C, Mazzanti CM, Proietti A, Koepsell H, Ferrannini E.

Diabetes Obes Metab. 2017 Sep;19(9):1289-1294. doi: 10.1111/dom.12970. Epub 2017 May 22.



Wang XX, Levi J, Luo Y, Myakala K, Herman-Edelstein M, Qiu L, Wang D, Peng Y, Grenz A, Lucia S, Dobrinskikh E, D'Agati VD, Koepsell H, Kopp JB, Rosenberg AZ, Levi M.

J Biol Chem. 2017 Mar 31;292(13):5335-5348. doi: 10.1074/jbc.M117.779520. Epub 2017 Feb 14.


Sodium-myoinositol cotransporter-1, SMIT1, mediates the production of reactive oxygen species induced by hyperglycemia in the heart.

Van Steenbergen A, Balteau M, Ginion A, Ferté L, Battault S, Ravenstein CM, Balligand JL, Daskalopoulos EP, Gilon P, Despa F, Despa S, Vanoverschelde JL, Horman S, Koepsell H, Berry G, Hue L, Bertrand L, Beauloye C.

Sci Rep. 2017 Jan 27;7:41166. doi: 10.1038/srep41166.


Response to "Tenofovir Disoproxil Fumarate Is Not an Inhibitor of Human Organic Cation Transporter 1".

Minuesa G, Albert C, Pastor-Anglada M, Martinez-Picado J, Koepsell H.

J Pharmacol Exp Ther. 2017 Feb;360(2):343-345. doi: 10.1124/jpet.116.239004. No abstract available.


Impact of Organic Cation Transporters (OCT-SLC22A) on Differential Diagnosis of Intrahepatic Lesions.

Visentin M, van Rosmalen BV, Hiller C, Bieze M, Hofstetter L, Verheij J, Kullak-Ublick GA, Koepsell H, Phoa SS, Tamai I, Bennink RJ, van Gulik TM, Stieger B.

Drug Metab Dispos. 2017 Feb;45(2):166-173. doi: 10.1124/dmd.116.072371. Epub 2016 Nov 30.


The Na+-D-glucose cotransporters SGLT1 and SGLT2 are targets for the treatment of diabetes and cancer.

Koepsell H.

Pharmacol Ther. 2017 Feb;170:148-165. doi: 10.1016/j.pharmthera.2016.10.017. Epub 2016 Oct 20. Review.


A Renal Olfactory Receptor Aids in Kidney Glucose Handling.

Shepard BD, Cheval L, Peterlin Z, Firestein S, Koepsell H, Doucet A, Pluznick JL.

Sci Rep. 2016 Oct 14;6:35215. doi: 10.1038/srep35215.


Expression of JAK3 Sensitive Na+ Coupled Glucose Carrier SGLT1 in Activated Cytotoxic T Lymphocytes.

Bhavsar SK, Singh Y, Sharma P, Khairnar V, Hosseinzadeh Z, Zhang S, Palmada M, Sabolic I, Koepsell H, Lang KS, Lang PA, Lang F.

Cell Physiol Biochem. 2016;39(3):1209-28. doi: 10.1159/000447827. Epub 2016 Sep 5.


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.


Role of Human Organic Cation Transporter 1 (hOCT1) Polymorphisms in Lamivudine (3TC) Uptake and Drug-Drug Interactions.

Arimany-Nardi C, Minuesa G, Keller T, Erkizia I, Koepsell H, Martinez-Picado J, Pastor-Anglada M.

Front Pharmacol. 2016 Jun 24;7:175. doi: 10.3389/fphar.2016.00175. eCollection 2016.


Erratum: Once daily administration of the SGLT2 inhibitor, empagliflozin, attenuates markers of renal fibrosis without improving albuminuria in diabetic db/db mice.

Gallo LA, Ward MS, Fotheringham AK, Zhuang A, Borg DJ, Flemming NB, Harvie BM, Kinneally TL, Yeh SM, McCarthy DA, Koepsell H, Vallon V, Pollock C, Panchapakesan U, Forbes JM.

Sci Rep. 2016 Jul 7;6:28124. doi: 10.1038/srep28124. No abstract available.


Once daily administration of the SGLT2 inhibitor, empagliflozin, attenuates markers of renal fibrosis without improving albuminuria in diabetic db/db mice.

Gallo LA, Ward MS, Fotheringham AK, Zhuang A, Borg DJ, Flemming NB, Harvie BM, Kinneally TL, Yeh SM, McCarthy DA, Koepsell H, Vallon V, Pollock C, Panchapakesan U, Forbes JM.

Sci Rep. 2016 May 26;6:26428. doi: 10.1038/srep26428. Erratum in: Sci Rep. 2016 Jul 07;6:28124.


Distribution of organic anion transporters NaDC3 and OAT1-3 along the human nephron.

Breljak D, Ljubojević M, Hagos Y, Micek V, Balen Eror D, Vrhovac Madunić I, Brzica H, Karaica D, Radović N, Kraus O, Anzai N, Koepsell H, Burckhardt G, Burckhardt BC, Sabolić I.

Am J Physiol Renal Physiol. 2016 Jul 1;311(1):F227-38. doi: 10.1152/ajprenal.00113.2016. Epub 2016 Apr 6.


Revisiting the physiological roles of SGLTs and GLUTs using positron emission tomography in mice.

Sala-Rabanal M, Hirayama BA, Ghezzi C, Liu J, Huang SC, Kepe V, Koepsell H, Yu A, Powell DR, Thorens B, Wright EM, Barrio JR.

J Physiol. 2016 Aug 1;594(15):4425-38. doi: 10.1113/JP271904. Epub 2016 May 10.


Sodium glucose cotransporter SGLT1 as a therapeutic target in diabetes mellitus.

Song P, Onishi A, Koepsell H, Vallon V.

Expert Opin Ther Targets. 2016 Sep;20(9):1109-25. doi: 10.1517/14728222.2016.1168808. Epub 2016 Apr 12. Review.


SGLT1 sugar transporter/sensor is required for post-oral glucose appetition.

Sclafani A, Koepsell H, Ackroff K.

Am J Physiol Regul Integr Comp Physiol. 2016 Apr 1;310(7):R631-9. doi: 10.1152/ajpregu.00432.2015. Epub 2016 Jan 20.


Regulation of intestinal SGLT1 by catestatin in hyperleptinemic type 2 diabetic mice.

Dominguez Rieg JA, Chirasani VR, Koepsell H, Senapati S, Mahata SK, Rieg T.

Lab Invest. 2016 Jan;96(1):98-111. doi: 10.1038/labinvest.2015.129. Epub 2015 Nov 9.


Role of SLC22A1 polymorphic variants in drug disposition, therapeutic responses, and drug-drug interactions.

Arimany-Nardi C, Koepsell H, Pastor-Anglada M.

Pharmacogenomics J. 2015 Dec;15(6):473-87. doi: 10.1038/tpj.2015.78. Epub 2015 Nov 3. Review.


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.


Role of the renal sympathetic nerve in renal glucose metabolism during the development of type 2 diabetes in rats.

Rafiq K, Fujisawa Y, Sherajee SJ, Rahman A, Sufiun A, Kobori H, Koepsell H, Mogi M, Horiuchi M, Nishiyama A.

Diabetologia. 2015 Dec;58(12):2885-98. doi: 10.1007/s00125-015-3771-9. Epub 2015 Oct 8.


Role of organic cation transporters in drug-drug interaction.

Koepsell H.

Expert Opin Drug Metab Toxicol. 2015;11(10):1619-33. doi: 10.1517/17425255.2015.1069274. Epub 2015 Jul 24. Review.


Ileal Interposition in Rats with Experimental Type 2 Like Diabetes Improves Glycemic Control Independently of Glucose Absorption.

Jurowich CF, Otto C, Rikkala PR, Wagner N, Vrhovac I, Sabolić I, Germer CT, Koepsell H.

J Diabetes Res. 2015;2015:490365. doi: 10.1155/2015/490365. Epub 2015 Jun 22.


Functional expression of sodium-glucose transporters in cancer.

Scafoglio C, Hirayama BA, Kepe V, Liu J, Ghezzi C, Satyamurthy N, Moatamed NA, Huang J, Koepsell H, Barrio JR, Wright EM.

Proc Natl Acad Sci U S A. 2015 Jul 28;112(30):E4111-9. doi: 10.1073/pnas.1511698112. Epub 2015 Jul 13.


Human organic cation transporter 1 (hOCT1) as a mediator of bendamustine uptake and cytotoxicity in chronic lymphocytic leukemia (CLL) cells.

Arimany-Nardi C, Montraveta A, Lee-Vergés E, Puente XS, Koepsell H, Campo E, Colomer D, Pastor-Anglada M.

Pharmacogenomics J. 2015 Aug;15(4):363-71. doi: 10.1038/tpj.2014.77. Epub 2015 Jan 13.


Absolute protein quantification allows differentiation of cell-specific metabolic routes and functions.

Wiśniewski JR, Koepsell H, Gizak A, Rakus D.

Proteomics. 2015 Apr;15(7):1316-25. doi: 10.1002/pmic.201400456. Epub 2015 Feb 17.


Localizations of Na(+)-D-glucose cotransporters SGLT1 and SGLT2 in human kidney and of SGLT1 in human small intestine, liver, lung, and heart.

Vrhovac I, Balen Eror D, Klessen D, Burger C, Breljak D, Kraus O, Radović N, Jadrijević S, Aleksic I, Walles T, Sauvant C, Sabolić I, Koepsell H.

Pflugers Arch. 2015 Sep;467(9):1881-98. doi: 10.1007/s00424-014-1619-7. Epub 2014 Oct 11.


The impact of high-fat diet on metabolism and immune defense in small intestine mucosa.

Wiśniewski JR, Friedrich A, Keller T, Mann M, Koepsell H.

J Proteome Res. 2015 Jan 2;14(1):353-65. doi: 10.1021/pr500833v. Epub 2014 Oct 23.


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.


The role of SGLT1 and GLUT2 in intestinal glucose transport and sensing.

Röder PV, Geillinger KE, Zietek TS, Thorens B, Koepsell H, Daniel H.

PLoS One. 2014 Feb 26;9(2):e89977. doi: 10.1371/journal.pone.0089977. eCollection 2014.


Does the haplotype Met408-Del420, which was apparently predictive for imatinib efficacy, really exist and how strongly may it affect OCT1 activity?

Tzvetkov MV, Seitz T, Bokelmann K, Mueller T, Brockmöller J, Koepsell H.

Blood. 2014 Feb 27;123(9):1427-9. doi: 10.1182/blood-2013-11-535864. No abstract available.


Sodium glucose cotransporter 1 ligand BLF501 as a novel tool for management of gastrointestinal mucositis.

Cardani D, Sardi C, La Ferla B, D'Orazio G, Sommariva M, Marcucci F, Olivero D, Tagliabue E, Koepsell H, Nicotra F, Balsari A, Rumio C.

Mol Cancer. 2014 Feb 5;13:23. doi: 10.1186/1476-4598-13-23.


Cellular uptake of imatinib into leukemic cells is independent of human organic cation transporter 1 (OCT1).

Nies AT, Schaeffeler E, van der Kuip H, Cascorbi I, Bruhn O, Kneba M, Pott C, Hofmann U, Volk C, Hu S, Baker SD, Sparreboom A, Ruth P, Koepsell H, Schwab M.

Clin Cancer Res. 2014 Feb 15;20(4):985-94. doi: 10.1158/1078-0432.CCR-13-1999. Epub 2013 Dec 18.


SGLT2 inhibitor empagliflozin reduces renal growth and albuminuria in proportion to hyperglycemia and prevents glomerular hyperfiltration in diabetic Akita mice.

Vallon V, Gerasimova M, Rose MA, Masuda T, Satriano J, Mayoux E, Koepsell H, Thomson SC, Rieg T.

Am J Physiol Renal Physiol. 2014 Jan;306(2):F194-204. doi: 10.1152/ajprenal.00520.2013. Epub 2013 Nov 13.


Increase in SGLT1-mediated transport explains renal glucose reabsorption during genetic and pharmacological SGLT2 inhibition in euglycemia.

Rieg T, Masuda T, Gerasimova M, Mayoux E, Platt K, Powell DR, Thomson SC, Koepsell H, Vallon V.

Am J Physiol Renal Physiol. 2014 Jan;306(2):F188-93. doi: 10.1152/ajprenal.00518.2013. Epub 2013 Nov 13.

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