SLC22A2

Summary

Gene Symbol: SLC22A2
Description: solute carrier family 22 member 2
Alias: OCT2, solute carrier family 22 member 2, organic cation transporter 2, solute carrier family 22 (organic cation transporter), member 2
Species: human
Products:     SLC22A2

Top Publications

  1. Ciarimboli G, Ludwig T, Lang D, Pavenstadt H, Koepsell H, Piechota H, et al. Cisplatin nephrotoxicity is critically mediated via the human organic cation transporter 2. Am J Pathol. 2005;167:1477-84 pubmed
    ..Here, we clearly identify the human organic cation transporter 2 (hOCT2) as the critical transporter for cis-platin nephrotoxicity in isolated human proximal tubules ..
  2. Song I, Shin H, Shim E, Jung I, Kim W, Shon J, et al. Genetic variants of the organic cation transporter 2 influence the disposition of metformin. Clin Pharmacol Ther. 2008;84:559-62 pubmed publisher
    Genetic variants of the organic cation transporter 2 (protein, OCT2; gene, SLC22A2) were evaluated for their contribution to the variations in the pharmacokinetics of metformin, especially to its renal elimination...
  3. Leabman M, Huang C, Kawamoto M, Johns S, Stryke D, Ferrin T, et al. Polymorphisms in a human kidney xenobiotic transporter, OCT2, exhibit altered function. Pharmacogenetics. 2002;12:395-405 pubmed
    ..study was to understand the relationship between variation in a gene encoding a major renal xenobiotic transporter, OCT2, and transporter function...
  4. Pelis R, Zhang X, Dangprapai Y, Wright S. Cysteine accessibility in the hydrophilic cleft of human organic cation transporter 2. J Biol Chem. 2006;281:35272-80 pubmed
    ..A hypothetical three-dimensional structure of OCT2 based on a homology model that used the Escherichia coli glycerol 3-phosphate transporter as a template has been ..
  5. Kang H, Song I, Shin H, Kim W, Lee C, Shim J, et al. Identification and functional characterization of genetic variants of human organic cation transporters in a Korean population. Drug Metab Dispos. 2007;35:667-75 pubmed
  6. Filipski K, Loos W, Verweij J, Sparreboom A. Interaction of Cisplatin with the human organic cation transporter 2. Clin Cancer Res. 2008;14:3875-80 pubmed publisher
    Cisplatin is predominantly eliminated in the urine through active secretion. As the solute carrier organic cation transporter 2 (OCT2) is highly expressed in the basolateral membrane of proximal tubules, we determined its contribution to ..
  7. Song I, Shin H, Shin J. Genetic variants of organic cation transporter 2 (OCT2) significantly reduce metformin uptake in oocytes. Xenobiotica. 2008;38:1252-62 pubmed
    ..model for the renal proximal tubule, and to investigate the effects of three non-synonymous genetic variants of OCT2 on the transport activity of metformin in vitro using an oocyte over-expression system. 2...
  8. Chen Y, Li S, Brown C, Cheatham S, Castro R, Leabman M, et al. Effect of genetic variation in the organic cation transporter 2 on the renal elimination of metformin. Pharmacogenet Genomics. 2009;19:497-504 pubmed publisher
    The goal of this study was to determine the effect of a genetic variant in the organic cation transporter 2 (OCT2), OCT2-808G/T, which results in an amino acid change, A270S, on the pharmacokinetics of the antidiabetic drug, metformin...
  9. Winter T, Elmquist W, Fairbanks C. OCT2 and MATE1 provide bidirectional agmatine transport. Mol Pharm. 2011;8:133-42 pubmed publisher
    ..The SLC-family organic cation transporters (OCT) OCT1 and OCT2 and multidrug and toxin extrusion transporter-1 (MATE1) are transport systems that may be of importance for the ..

More Information

Publications126 found, 100 shown here

  1. Elsby R, Chidlaw S, Outteridge S, Pickering S, Radcliffe A, Sullivan R, et al. Mechanistic in vitro studies confirm that inhibition of the renal apical efflux transporter multidrug and toxin extrusion (MATE) 1, and not altered absorption, underlies the increased metformin exposure observed in clinical interactions with cimetidi. Pharmacol Res Perspect. 2017;5: pubmed publisher
    ..transporters are responsible for AUC increases, in vitro inhibitory potencies against metformin transport by human OCT2, multidrug and toxin extrusion (MATE) 1 and MATE2-K were determined...
  2. Yang Y, Zhang D, Liu J, Hu L, Xue Q, Ding X, et al. Wuling San protects kidney dysfunction by inhibiting renal TLR4/MyD88 signaling and NLRP3 inflammasome activation in high fructose-induced hyperuricemic mice. J Ethnopharmacol. 2015;169:49-59 pubmed publisher
    ..G member 2 (ABCG2) and organic anion transporter 1 (OAT1), as well as organic cation transporter 1 (OCT1) and OCT2 in mice...
  3. Wang R, Ma C, Zhou F, Kong L. Siwu decoction attenuates oxonate-induced hyperuricemia and kidney inflammation in mice. Chin J Nat Med. 2016;14:499-507 pubmed publisher
    ..transporters 1 (OAT1), ATP-binding cassette subfamily G member 2 (ABCG2), organic cation transporter 1 (OCT1), OCT2, organic cation/carnitine transporter 1 (OCTN1), OCNT2, Nod-like receptor family, pyrin domain containing 3 (NLRP3),..
  4. Mihaljević I, Popovic M, Zaja R, Maraković N, Sinko G, Smital T. Interaction between the zebrafish (Danio rerio) organic cation transporter 1 (Oct1) and endo- and xenobiotics. Aquat Toxicol. 2017;187:18-28 pubmed publisher
    ..with three co-orthologs identified in humans (OCT1, 2 and 3), and two Oct orthologs in zebrafish (Oct1 and Oct2)...
  5. Chen Y, Chen C, Yan W, Ge H, Kong L. Anti-hyperuricemic and anti-inflammatory actions of vaticaffinol isolated from Dipterocarpus alatus in hyperuricemic mice. Chin J Nat Med. 2017;15:330-340 pubmed publisher
    ..1 (URAT1), glucose transporter 9 (GLUT9), organic anion transporter 1 (OAT1), organic cation transporter 1 (OCT1), OCT2, organic cation/carnitine transporter 1 (OCTN1), and OCTN2 in hyperuricemic mice...
  6. Shemesh C, Yu R, Warren M, Liu M, Jahic M, Nichols B, et al. Assessment of the Drug Interaction Potential of Unconjugated and GalNAc3-Conjugated 2'-MOE-ASOs. Mol Ther Nucleic Acids. 2017;9:34-47 pubmed publisher
    ..1B1 (OATP1B1), and OATP1B3; three renal uptake transporters, organic anion transporter 1 (OAT1), OAT3, and OCT2; and three efflux transporters, P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and bile salt ..
  7. Parvez M, Kaisar N, Shin H, Lee Y, Shin J. Comprehensive Substrate Characterization of 22 Antituberculosis Drugs for Multiple Solute Carrier (SLC) Uptake Transporters In Vitro. Antimicrob Agents Chemother. 2018;62: pubmed publisher
    ..1 ± 15.6, 212.0 ± 20.1, 336.8 ± 20.1, and 455.0 ± 28 μM for organic cation transporter 1 (OCT1), OCT2, OCTN1, and OCTN2, respectively. Similarly, the Km of prothionamide was 805.8 ± 23...
  8. Mayati A, Bruyère A, Moreau A, Jouan E, Denizot C, Parmentier Y, et al. Protein Kinase C-Independent Inhibition of Organic Cation Transporter 1 Activity by the Bisindolylmaleimide Ro 31-8220. PLoS ONE. 2015;10:e0144667 pubmed publisher
    ..such as multidrug and toxin extrusion protein (MATE) 1 and MATE2-K, whereas, by contrast, it stimulated that of OCT2. Taken together, these data extend the nature of cellular off-targets of the BIM Ro 31-8220 to OCT1 and other ..
  9. Sekhar G, Georgian A, Sanderson L, Vizcay Barrena G, Brown R, Muresan P, et al. Organic cation transporter 1 (OCT1) is involved in pentamidine transport at the human and mouse blood-brain barrier (BBB). PLoS ONE. 2017;12:e0173474 pubmed publisher
    ..3 cell lines, respectively. Results revealed that both cell lines expressed the organic cation transporters (OCT1, OCT2 and OCT3), however, P-gp was only expressed in hCMEC/D3 cells. Polarised expression of OCT1 was also observed...
  10. Wang Z, Liu Y, Liu G, Lu H, Mao C. l-Carnitine and heart disease. Life Sci. 2018;194:88-97 pubmed publisher
    ..This review describes the mechanism of action, metabolism and pharmacokinetics of l-carnitine. It specifically emphasizes upon the beneficial role of l-carnitine in cardiomyopathy. ..
  11. Lee S, Lee H, Park G, Oh S, Oh D. Dual actions on gout flare and acute kidney injury along with enhanced renal transporter activities by Yokuininto, a Kampo medicine. BMC Complement Altern Med. 2019;19:57 pubmed publisher
    ..Renal transporter uptake assays were performed using HEK293 cells overexpressing OAT1, OCT2 or OAT3, MDCKII cells overexpressing BCRP, and Xenopus oocytes overexpressing OAT3 or URAT1...
  12. Wang S, Fang Y, Yu X, Guo L, Zhang X, Xia D. The flavonoid-rich fraction from rhizomes of Smilax glabra Roxb. ameliorates renal oxidative stress and inflammation in uric acid nephropathy rats through promoting uric acid excretion. Biomed Pharmacother. 2019;111:162-168 pubmed publisher
    ..of ATP-binding cassette transporter G2 (ABCG2), organic anion transporter 1 (OAT1), organic anion transporters 2 (OCT2) and organic cation/carnitine transporters 2 (OCTN2) expression...
  13. Rizk M, Houle R, Chan G, Hafey M, Rhee E, Chu X. Raltegravir has a low propensity to cause clinical drug interactions through inhibition of major drug transporters: an in vitro evaluation. Antimicrob Agents Chemother. 2014;58:1294-301 pubmed publisher
    ..the maximum concentration of drug in plasma (Cmax) at the clinical 400-mg dose and did not inhibit organic cation transporter 2 (OCT2)...
  14. Qian X, Wang X, Luo J, Liu Y, Pang J, Zhang H, et al. Hypouricemic and nephroprotective roles of anthocyanins in hyperuricemic mice. Food Funct. 2019;10:867-878 pubmed publisher
    ..IL-1β) and regulated the expression of renal urate transporters URAT1, GLUT9, ABCG2, OAT1, OAT3, OCT1, OCT2, OCTN1 and OCTN2...
  15. Martovetsky G, Tee J, Nigam S. Hepatocyte nuclear factors 4α and 1α regulate kidney developmental expression of drug-metabolizing enzymes and drug transporters. Mol Pharmacol. 2013;84:808-23 pubmed publisher
    ..Fmo1, Cyp2d2, Cyp2d4, Nqo2, as well as organic cation transporters and organic anion transporters Slc22a1 (Oct1), Slc22a2 (Oct2), Slc22a6 (Oat1), Slc22a8 (Oat3), and Slc47a1 (Mate1)...
  16. Thevenod F, Fels J, Lee W, Zarbock R. Channels, transporters and receptors for cadmium and cadmium complexes in eukaryotic cells: myths and facts. Biometals. 2019;: pubmed publisher
    ..Cd2+ flux occurs through the influx carrier OCT2/SLC22A2, efflux MATE proteins SLC47A1/A2, the efflux ATPase ABCB1, and RME of Cd2+-metallothionein by the ..
  17. Takano H, Ito S, Zhang X, Ito H, Zhang M, Suzuki H, et al. Possible Role of Organic Cation Transporters in the Distribution of [11C]Sulpiride, a Dopamine D2 Receptor Antagonist. J Pharm Sci. 2017;106:2558-2565 pubmed publisher
    ..In conclusion, we found that sulpiride is a substrate of OCT1, OCT2, MATE1, and MATE2-K, and this suggests that [11C]sulpiride would be a useful radioligand to investigate ..
  18. Rivero A, Domingo P. [Safety profile of dolutegravir]. Enferm Infecc Microbiol Clin. 2015;33 Suppl 1:9-13 pubmed publisher
    ..This increase is due to inhibition of tubular creatinine secretion through the OCT2 receptor and does not lead to a real decrease in estimated glomerular filtration rate with algorithms that include ..
  19. Gao H, Zhang S, Hu T, Qu X, Zhai J, Zhang Y, et al. Omeprazole protects against cisplatin-induced nephrotoxicity by alleviating oxidative stress, inflammation, and transporter-mediated cisplatin accumulation in rats and HK-2 cells. Chem Biol Interact. 2019;297:130-140 pubmed publisher
    ..OME reduced CP cellular uptake through organic cation transporters 2 (OCT2) and the prompt efflux of CP by P-glycoprotein (P-gp), thereby reducing the accumulation of CP in kidney tissue and ..
  20. Johnston R, Rawling T, Chan T, Zhou F, Murray M. Selective inhibition of human solute carrier transporters by multikinase inhibitors. Drug Metab Dispos. 2014;42:1851-7 pubmed publisher
    ..cation transporter 1 (OCT1) were inhibited by most MKIs, whereas substrate uptake by OATP1B1, OAT1, 2, and 4, OCT2 and 3, and organic zwitterion/cation transporter 1 (OCTN1) was less susceptible to inhibition; OCTN2 was also ..
  21. Kazmi F, Yerino P, McCoy C, Parkinson A, Buckley D, Ogilvie B. An Assessment of the In Vitro Inhibition of Cytochrome P450 Enzymes, UDP-Glucuronosyltransferases, and Transporters by Phosphodiester- or Phosphorothioate-Linked Oligonucleotides. Drug Metab Dispos. 2018;46:1066-1074 pubmed publisher
    ..polypeptide OATP1B1 and OATP1B3, organic anion transporters OAT1 and OAT3, and organic cation transporter OCT2 (IC50 values of 12-29 μM), but not OCT1 or the efflux transporters breast cancer resistance ..
  22. Marcho C, Bevilacqua A, Tremblay K, Mager J. Tissue-specific regulation of Igf2r/Airn imprinting during gastrulation. Epigenetics Chromatin. 2015;8:10 pubmed publisher
    ..One imprinted cluster includes the maternally expressed Igf2r, Slc22a2, and Slc22a3 genes and the paternally expressed long non-coding RNA (lncRNA) Airn...
  23. Kashyap M, Pore S, de Groat W, Chermansky C, Yoshimura N, Tyagi P. BDNF Overexpression in Bladder Induces Neuronal Changes To Mediate Bladder Overactivity. Am J Physiol Renal Physiol. 2017;:ajprenal.00386.2017 pubmed publisher
    ..and upregulation of choline acetyltransferase (ChAT), vesicular acetylcholine transporter (VAChT), transporter Oct2 and ?1 receptors...
  24. Mamidi R, Dallas S, Sensenhauser C, Lim H, Scheers E, Verboven P, et al. In vitro and physiologically-based pharmacokinetic based assessment of drug-drug interaction potential of canagliflozin. Br J Clin Pharmacol. 2017;83:1082-1096 pubmed publisher
    ..isoforms OATP1B1, OATP1B3, organic anion transporters OAT1 and OAT3, and organic cationic transporters OCT1, and OCT2)...
  25. Ribera E, Podzamczer D. [Mechanisms of action, pharmacology and interactions of dolutegravir]. Enferm Infecc Microbiol Clin. 2015;33 Suppl 1:2-8 pubmed publisher
    ..Dolutegravir can reduce renal tubule secretion of substances excreted via OCT2, with a slight initial increase in creatinine, with no risk of renal toxicity...
  26. Reese M, Savina P, Generaux G, Tracey H, Humphreys J, Kanaoka E, et al. In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor. Drug Metab Dispos. 2013;41:353-61 pubmed publisher
    ..Further, DTG did not induce CYP1A2, 2B6, or 3A4 mRNA in vitro using human hepatocytes. DTG does inhibit the renal OCT2 (IC(50) = 1...
  27. Jansen J, Schophuizen C, Wilmer M, Lahham S, Mutsaers H, Wetzels J, et al. A morphological and functional comparison of proximal tubule cell lines established from human urine and kidney tissue. Exp Cell Res. 2014;323:87-99 pubmed publisher
    ..01 and p<0.05, respectively). Expression of the influx carrier Organic Cation Transporter 2 (OCT-2), and the efflux pumps P-glycoprotein (P-gp), Multidrug Resistance Protein 4 (MRP4) and Breast ..
  28. Balaratnasingam C, An D, Sakurada Y, Lee C, Lee A, McAllister I, et al. Comparisons Between Histology and Optical Coherence Tomography Angiography of the Periarterial Capillary-Free Zone. Am J Ophthalmol. 2018;189:55-64 pubmed publisher
    ..1.5.0.15909; Zeiss Meditec, Inc, Dublin, California, USA), Heidelberg Spectralis OCT2 (Family acquisition module 6.7.21.0; Heidelberg Engineering, Heidelberg, Germany), and DRI-OCT Triton (Ver. 1.1...
  29. Lenis Y, Elmetwally M, Tang W, Satterfield C, Dunlap K, Wu G, et al. Functional roles of agmatinase during the peri-implantation period of pregnancy in sheep. Amino Acids. 2018;50:293-308 pubmed publisher
    ..Moreover, inhibition of translational of both ODC1 and AGMAT mRNAs increased expression of ADC, SLC22A1, SLC22A2, and SLC22A3 mRNAs, as well as abundances of agmatine, putrescine, spermindine, and spermine in conceptus tissue...
  30. Murase T, Fujita A, Ueno H, Park J, Yano T, Hoshikawa M, et al. A case of age-related EBV-associated B-cell lymphoproliferative disorder metachronously showing two distinct morphologic appearances, one of a polymorphic disease resembling classical Hodgkin lymphoma, and the other of a large-cell lymphoma. Int J Hematol. 2009;89:80-85 pubmed publisher
    ..ruled out, because neoplastic giant cells resembling Hodgkin and Reed-Sternberg (HRS) cells were positive for both Oct2 and BOB.1, which has not been reported in CHL...
  31. Ma Y, Huang J, Shao Y, Ma K, Zhang G, Zhou Y, et al. Inhibitory effect of atenolol on urinary excretion of metformin via down-regulating multidrug and toxin extrusion protein 1 (rMate1) expression in the kidney of rats. Eur J Pharm Sci. 2015;68:18-26 pubmed publisher
    ..Western blotting and immunohistochemical analysis were used to evaluate the renal expression of rat organic cation transporter 2 (rOct2) and multidrug and toxin extrusion protein 1 (rMate1)...
  32. Visentin M, van Rosmalen B, Hiller C, Bieze M, Hofstetter L, Verheij J, et al. Impact of Organic Cation Transporters (OCT-SLC22A) on Differential Diagnosis of Intrahepatic Lesions. Drug Metab Dispos. 2017;45:166-173 pubmed publisher
    ..HEK293 cells overexpressing OCT1, OCT2, or OCT3 showed higher intracellular levels of FCH in comparison with wild-type cells...
  33. Burckhardt G, Wolff N. Structure of renal organic anion and cation transporters. Am J Physiol Renal Physiol. 2000;278:F853-66 pubmed
    ..properties of organic anion transporters (OAT1, OAT2, OAT3) and organic cation transporters (OCTN1, OCTN2, OCT1, OCT2, OCT3), some of which are involved in renal proximal tubular organic anion and cation secretion...
  34. Otter M, Oswald S, Siegmund W, Keiser M. Effects of frequently used pharmaceutical excipients on the organic cation transporters 1-3 and peptide transporters 1/2 stably expressed in MDCKII cells. Eur J Pharm Biopharm. 2017;112:187-195 pubmed publisher
    ..of frequently used pharmaceutical excipients on the transport activity of organic cation transporters OCT1, OCT2 and OCT3 and the peptide transporters PEPT1 and PEPT2...
  35. Chen Y, Zhang S, Sorani M, Giacomini K. Transport of paraquat by human organic cation transporters and multidrug and toxic compound extrusion family. J Pharmacol Exp Ther. 2007;322:695-700 pubmed
    ..These transporters may play an important role in the accumulation and renal excretion of PQ, and they may serve as molecular targets for the prevention and treatment of PQ-induced nephrotoxicity. ..
  36. Vermeer L, Isringhausen C, Ogilvie B, Buckley D. Evaluation of Ketoconazole and Its Alternative Clinical CYP3A4/5 Inhibitors as Inhibitors of Drug Transporters: The In Vitro Effects of Ketoconazole, Ritonavir, Clarithromycin, and Itraconazole on 13 Clinically-Relevant Drug Transporters. Drug Metab Dispos. 2016;44:453-9 pubmed publisher
    ..hydroxy-, keto-, and N-desalkyl itraconazole) toward 13 drug transporters (OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, MATE1, MATE2-K, P-gp, BCRP, MRP2, MRP3, and BSEP) were systematically assessed in transporter-expressing HEK-293 ..
  37. Salomon J, Gausterer J, Yahara T, Hosoya K, Huwer H, Hittinger M, et al. Organic cation transporter function in different in vitro models of human lung epithelium. Eur J Pharm Sci. 2015;80:82-8 pubmed publisher
    ..RNAi experiments in A549 cells confirmed that TEA uptake was mainly facilitated by OCT1 and OCT2. Co-incubation studies using pharmacological OCT modulators suggested that organic cation uptake pathways share ..
  38. Hodson D, Shaffer A, Xiao W, Wright G, Schmitz R, Phelan J, et al. Regulation of normal B-cell differentiation and malignant B-cell survival by OCT2. Proc Natl Acad Sci U S A. 2016;113:E2039-46 pubmed publisher
    The requirement for the B-cell transcription factor OCT2 (octamer-binding protein 2, encoded by Pou2f2) in germinal center B cells has proved controversial...
  39. Cheung K, Hsueh C, Zhao P, Meyer T, Zhang L, Huang S, et al. The Effect of Uremic Solutes on the Organic Cation Transporter 2. J Pharm Sci. 2017;106:2551-2557 pubmed publisher
    ..The goal of this study is to evaluate the effect of uremic solutes on the organic cation transporter, OCT2, which plays a key role in the renal secretion of many basic drugs...
  40. Barendt W, Wright S. The human organic cation transporter (hOCT2) recognizes the degree of substrate ionization. J Biol Chem. 2002;277:22491-6 pubmed
    The organic cation transporter, OCT2, plays a role in renal secretion of a broad array of weak bases...
  41. Mukherjee M, Pritchard D, Bosquillon C. Evaluation of air-interfaced Calu-3 cell layers for investigation of inhaled drug interactions with organic cation transporters in vitro. Int J Pharm. 2012;426:7-14 pubmed publisher
    ..21 day old Calu-3 layers expressed OCT1, OCT3, OCTN1 and OCTN2 whereas OCT2 could not be detected...
  42. Cho S, Chung J. The MATE1 rs2289669 polymorphism affects the renal clearance of metformin following ranitidine treatment. Int J Clin Pharmacol Ther. 2016;54:253-62 pubmed publisher
    Human multidrug and toxin extrusion member 1 (MATE1, SLC47A1) and Organic Cation Transporter 2 (OCT2, SLC22A2) play important roles in the renal elimination of various pharmacologic agents, including the anti-diabetic drug metformin...
  43. Bergagnini Kolev M, Hebert M, Easterling T, Lin Y. Pregnancy Increases the Renal Secretion of N1-methylnicotinamide, an Endogenous Probe for Renal Cation Transporters, in Patients Prescribed Metformin. Drug Metab Dispos. 2017;45:325-329 pubmed publisher
    ..1-NMN) has been investigated as an endogenous probe for the renal transporter activity of organic cation transporter 2 (OCT2) and multidrug and toxin extrusion proteins 1 and 2-K (MATE1 and MATE2-K)...
  44. Ikemura K, Oshima K, Enokiya T, Okamoto A, Oda H, Mizuno T, et al. Co-administration of proton pump inhibitors ameliorates nephrotoxicity in patients receiving chemotherapy with cisplatin and fluorouracil: a retrospective cohort study. Cancer Chemother Pharmacol. 2017;79:943-949 pubmed publisher
    ..CDDP) is its dose-limiting side effect, and is caused by renal accumulation of CDDP mainly via organic cation transporter 2 (OCT2)...
  45. Nakada T, Kudo T, Kume T, Kusuhara H, Ito K. Quantitative analysis of elevation of serum creatinine via renal transporter inhibition by trimethoprim in healthy subjects using physiologically-based pharmacokinetic model. Drug Metab Pharmacokinet. 2018;33:103-110 pubmed publisher
    ..inhibition by trimethoprim on tubular secretion of creatinine via renal transporters such as organic cation transporter 2 (OCT2), OCT3, multidrug and toxin extrusion protein 1 (MATE1), and MATE2-K...
  46. Luo W, Li S, Peng B, Ye Y, Deng X, Yao K. Embryonic stem cells markers SOX2, OCT4 and Nanog expression and their correlations with epithelial-mesenchymal transition in nasopharyngeal carcinoma. PLoS ONE. 2013;8:e56324 pubmed publisher
    ..Additionally, cancer cells in the invasive front of NPC acquiring ESCs-like features should be maintained by vascular niches. ..
  47. Chowdhury S, Yung E, Pintilie M, Muaddi H, Chaib S, Yeung M, et al. MATE2 Expression Is Associated with Cancer Cell Response to Metformin. PLoS ONE. 2016;11:e0165214 pubmed publisher
    ..The expression of OCT1 correlated with expression of both OCT2 and OCT3...
  48. Bruyère A, Hubert C, Le Vee M, Chedik L, Sayyed K, Stieger B, et al. Inhibition of SLC drug transporter activities by environmental bisphenols. Toxicol In Vitro. 2017;40:34-44 pubmed publisher
    ..contrast, activities of other transporters were not impacted (MATE2-K) or were stimulated (notably OCT1 by BPS and OCT2 by BPF)...
  49. Wagner D, Sager J, Duan H, Isoherranen N, Wang J. Interaction and Transport of Methamphetamine and its Primary Metabolites by Organic Cation and Multidrug and Toxin Extrusion Transporters. Drug Metab Dispos. 2017;45:770-778 pubmed publisher
    ..Our studies suggest the involvement of the renal OCT2/MATE pathway in tubular secretion of methamphetamine and its major metabolites and the potential of drug-drug ..
  50. Cetinkaya I, Ciarimboli G, Yalçinkaya G, Mehrens T, Velic A, Hirsch J, et al. Regulation of human organic cation transporter hOCT2 by PKA, PI3K, and calmodulin-dependent kinases. Am J Physiol Renal Physiol. 2003;284:F293-302 pubmed
    ..In conclusion, we demonstrate that the hOCT2 is inhibited by PI3K and PKA and activated by a CaM-dependent signaling pathway, probably via a change in substrate affinity. ..
  51. Tzvetkov M, Vormfelde S, Balen D, Meineke I, Schmidt T, Sehrt D, et al. The effects of genetic polymorphisms in the organic cation transporters OCT1, OCT2, and OCT3 on the renal clearance of metformin. Clin Pharmacol Ther. 2009;86:299-306 pubmed publisher
    ..We explored metformin pharmacokinetics in relation to genetic variations in OCT1, OCT2, OCT3, OCTN1, and MATE1 in 103 healthy male Caucasians. Renal clearance varied 3...
  52. Knop J, Hoier E, Ebner T, Fromm M, Müller F. Renal tubular secretion of pramipexole. Eur J Pharm Sci. 2015;79:73-8 pubmed publisher
    ..Previously the organic cation transporter 2 (OCT2) was shown to be involved in the uptake of pramipexole by renal tubular cells, while the ..
  53. Yu X, Zhang X, Jin L, Feng G. CO adsorption, oxidation and carbonate formation mechanisms on Fe3O4 surfaces. Phys Chem Chem Phys. 2017;19:17287-17299 pubmed publisher
    ..It has been found that more than one CO can coadsorb on one surface iron atom on both Fetet1 and Feoct2 terminations of Fe3O4(111)...
  54. Benzi J, Yamamoto P, Stevens J, Baviera A, de Moraes N. The role of organic cation transporter 2 inhibitor cimetidine, experimental diabetes mellitus and metformin on gabapentin pharmacokinetics in rats. Life Sci. 2018;200:63-68 pubmed publisher
    We investigated the influence of diabetes mellitus (DM), glycemic control with insulin, cimetidine (Oct2 inhibitor) and metformin (Oct2 substrate) on the kinetic disposition of GAB in rats...
  55. Sallinen R, Kaunisto M, Forsblom C, Thomas M, Fagerudd J, Pettersson Fernholm K, et al. Association of the SLC22A1, SLC22A2, and SLC22A3 genes encoding organic cation transporters with diabetic nephropathy and hypertension. Ann Med. 2010;42:296-304 pubmed publisher
    ..Our aim was to find out if single nucleotide polymorphisms (SNPs) within the SLC22A1, SLC22A2, and SLC22A3 genes encoding organic cation transporters (OCTs) associate with DN or hypertension...
  56. Park T, Kim J, Bae J, Park B, Cheong H, Chun J, et al. Possible association of SLC22A2 polymorphisms with aspirin-intolerant asthma. Int Arch Allergy Immunol. 2011;155:395-402 pubmed publisher
    ..Solute carrier family 22, member 2 (SLC22A2), also known as organic cation transporter 2 (OCT2), is predominantly expressed in the luminal membrane of airway epithelial cells and has been ..
  57. Nigam S, Wu W, Bush K, Hoenig M, Blantz R, Bhatnagar V. Handling of Drugs, Metabolites, and Uremic Toxins by Kidney Proximal Tubule Drug Transporters. Clin J Am Soc Nephrol. 2015;10:2039-49 pubmed publisher
    ..With an emphasis on OAT1 (SLC22A6), the closely related OAT3 (SLC22A8), and OCT2 (SLC22A2), we explore the implications of recent in vitro, in vivo, and clinical data pertinent to the kidney...
  58. Li L, Song F, Weng Y, Yang X, Wang K, Lei H, et al. Role of OCT2 and MATE1 in renal disposition and toxicity of nitidine chloride. Br J Pharmacol. 2016;173:2543-54 pubmed publisher
    ..The aim of the present study was to evaluate the role of organic cation transporter 2 (OCT2) and multidrug and toxin extrusion 1 (MATE1) in the renal disposition and nephrotoxicity of NC...
  59. Martínez Guerrero L, Morales M, Ekins S, Wright S. Lack of Influence of Substrate on Ligand Interaction with the Human Multidrug and Toxin Extruder, MATE1. Mol Pharmacol. 2016;90:254-64 pubmed publisher
    ..In summary, in contrast to the behavior observed with some other multidrug transporters, including OCT2, the results suggest that substrate identity exerts comparatively little influence on ligand interaction with MATE1. ..
  60. Soodvilai S, Soodvilai S, Chatsudthipong V, Ngawhirunpat T, Rojanarata T, Opanasopit P. Interaction of pharmaceutical excipients with organic cation transporters. Int J Pharm. 2017;520:14-20 pubmed publisher
    ..12, 50±1.26, 106.00±1.20?g/ml, respectively, while the IC50 values for OCT2 were 295±1.48, 42±1.15, 185±1.20?g/ml, respectively...
  61. Severance A, Sandoval P, Wright S. Correlation between Apparent Substrate Affinity and OCT2 Transport Turnover. J Pharmacol Exp Ther. 2017;362:405-412 pubmed publisher
    Organic cation (OC) transporter 2 (OCT2) mediates the first step in the renal secretion of many cationic drugs: basolateral uptake from blood into proximal tubule cells...
  62. Fukushima Uesaka H, Maekawa K, Ozawa S, Komamura K, Ueno K, Shibakawa M, et al. Fourteen novel single nucleotide polymorphisms in the SLC22A2 gene encoding human organic cation transporter (OCT2). Drug Metab Pharmacokinet. 2004;19:239-44 pubmed
    Thirty-three genetic variations including fourteen novel ones were found in the SLC22A2 gene from 116 Japanese individuals...
  63. Katz D, Carr R, Grimm D, Xiong H, Holley Shanks R, Mueller T, et al. Organic anion transporting polypeptide 1B1 activity classified by SLCO1B1 genotype influences atrasentan pharmacokinetics. Clin Pharmacol Ther. 2006;79:186-96 pubmed
    ..Increased exposures of OATP1B1 substrates might be expected in individuals who have the poor transporter phenotype or are treated with an OATP1B1 inhibitor. ..
  64. Yin J, Duan H, Shirasaka Y, Prasad B, Wang J. Atenolol Renal Secretion Is Mediated by Human Organic Cation Transporter 2 and Multidrug and Toxin Extrusion Proteins. Drug Metab Dispos. 2015;43:1872-81 pubmed publisher
    ..Together, our data support that atenolol tubular secretion is mediated through the hOCT2/hMATEs secretion pathway and suggest a significant role of organic cation transporters in the disposition of an important antihypertensive drug. ..
  65. Liu G, Wen J, Guo D, Wang Z, Hu X, Tang J, et al. The effects of rabeprazole on metformin pharmacokinetics and pharmacodynamics in Chinese healthy volunteers. J Pharmacol Sci. 2016;132:244-248 pubmed publisher
    ..were carried out and showed that the half maximal inhibitory concentration (IC50) of rabeprazole on OCT2-mediated metformin transport was 26...
  66. McCormick A, Swaisland H. In vitro assessment of the roles of drug transporters in the disposition and drug-drug interaction potential of olaparib. Xenobiotica. 2017;47:903-915 pubmed publisher
    ..9??M), but limited inhibition of OATP1B3 (25% at 100??M); inhibition of the renal uptake transporters OCT2 (IC50 19.9??M) and OAT3 (IC50 18.4??M), but limited inhibition of OAT1 (13...
  67. Strobel J, Müller F, Zolk O, Endreß B, Konig J, Fromm M, et al. Transport of asymmetric dimethylarginine (ADMA) by cationic amino acid transporter 2 (CAT2), organic cation transporter 2 (OCT2) and multidrug and toxin extrusion protein 1 (MATE1). Amino Acids. 2013;45:989-1002 pubmed publisher
    ..of the human cationic amino acid transporters 2A (CAT2A, SLC7A2A) and 2B (CAT2B, SLC7A2B), the organic cation transporter 2 (OCT2, SLC22A2), and the multidrug and toxin extrusion protein 1 (MATE1, SLC47A1)...
  68. Meyer M, Seitz T, Brockmoller J, Tzvetkov M. Effects of genetic polymorphisms on the OCT1 and OCT2-mediated uptake of ranitidine. PLoS ONE. 2017;12:e0189521 pubmed publisher
    ..Ranitidine was reported to be a substrate of the organic cation transporters OCT1 and OCT2. The hepatic transporter OCT1 is highly genetically variable...
  69. Pelis R, Suhre W, Wright S. Functional influence of N-glycosylation in OCT2-mediated tetraethylammonium transport. Am J Physiol Renal Physiol. 2006;290:F1118-26 pubmed
    b>OCT2, an organic cation transporter critical for removal of many drugs and toxins from the body, contains consensus sites for N-glycosylation at amino acid position 71, 96, and 112...
  70. Tarasova L, Kalnina I, Geldnere K, Bumbure A, Ritenberga R, Nikitina Zake L, et al. Association of genetic variation in the organic cation transporters OCT1, OCT2 and multidrug and toxin extrusion 1 transporter protein genes with the gastrointestinal side effects and lower BMI in metformin-treated type 2 diabetes patients. Pharmacogenet Genomics. 2012;22:659-66 pubmed publisher
    ..So far, the number of polymorphisms in SLC22A1, SLC22A2, and SLC47A1 genes coding for organic cation transporter 1 (OCT1), OCT2, and multidrug and toxin extrusion ..
  71. Huang D, Wang C, Duan Y, Meng Q, Liu Z, Huo X, et al. Targeting Oct2 and P53: Formononetin prevents cisplatin-induced acute kidney injury. Toxicol Appl Pharmacol. 2017;326:15-24 pubmed publisher
    ..Formononetin decreased expression of organic cation transporter 2 (Oct2) and increased the expressions of multidrug resistance-associated proteins (Mrps), which might ..
  72. Jeang K, Chun R, Lin N, Gatignol A, Glabe C, Fan H. In vitro and in vivo binding of human immunodeficiency virus type 1 Tat protein and Sp1 transcription factor. J Virol. 1993;67:6224-33 pubmed
    ..These experiments extend previous genetic experiments and suggest a direct interaction between Tat and Sp1 during transactivation...
  73. Filipski K, Mathijssen R, Mikkelsen T, Schinkel A, Sparreboom A. Contribution of organic cation transporter 2 (OCT2) to cisplatin-induced nephrotoxicity. Clin Pharmacol Ther. 2009;86:396-402 pubmed publisher
    ..b>Organic cation transporter 2 (OCT2) has been implicated in the cellular uptake of cisplatin, but its role in cisplatin-induced ..
  74. Iwata K, Aizawa K, Kamitsu S, Jingami S, Fukunaga E, Yoshida M, et al. Effects of genetic variants in SLC22A2 organic cation transporter 2 and SLC47A1 multidrug and toxin extrusion 1 transporter on cisplatin-induced adverse events. Clin Exp Nephrol. 2012;16:843-51 pubmed publisher
    ..In the kidney, CDDP is taken up into the renal proximal tubular cells mainly via SLC22A2 organic cation transporter 2 (OCT2) and secreted into lumen via other transporters including SLC47A1 multidrug and toxin extrusion 1 ..
  75. Sauzay C, White Koning M, Hennebelle I, Deluche T, Delmas C, Imbs D, et al. Inhibition of OCT2, MATE1 and MATE2-K as a possible mechanism of drug interaction between pazopanib and cisplatin. Pharmacol Res. 2016;110:89-95 pubmed publisher
    We hypothesized that pazopanib is an inhibitor of cisplatin renal transporters OCT2, MATE1 and MATE2-K based on previous studies demonstrating an interaction between tyrosine kinase inhibitors and these transporters...
  76. Streeter A, Faria E. Analysis of the variability of the pharmacokinetics of multiple drugs in young adult and elderly subjects and its implications for acceptable daily exposures and cleaning validation limits. Int J Hyg Environ Health. 2017;220:659-672 pubmed publisher
    ..subjects for the 10 compounds which show the greatest separation are different in almost every case, involving the OCT2 transporter, glucuronidation, hydrolysis, CYP1A2, CYP2A6, CYP2C19, CYP2D6, CYP3A4 or CYP3A5...
  77. Verhaagh S, Schweifer N, Barlow D, Zwart R. Cloning of the mouse and human solute carrier 22a3 (Slc22a3/SLC22A3) identifies a conserved cluster of three organic cation transporters on mouse chromosome 17 and human 6q26-q27. Genomics. 1999;55:209-18 pubmed
    ..Igf2r and Plg genes in close association with two additional members of the Slc22a gene family, mouse Slc22a1 and Slc22a2. A partial cDNA sequence of the human SLC22A3 gene was reconstituted from sequenced EST clones...
  78. Burger H, Zoumaro Djayoon A, Boersma A, Helleman J, Berns E, Mathijssen R, et al. Differential transport of platinum compounds by the human organic cation transporter hOCT2 (hSLC22A2). Br J Pharmacol. 2010;159:898-908 pubmed publisher
    ..As decreased drug accumulation is a key mechanism of platinum resistance, SLCs may also contribute to the development of resistance. Here, we define the role of hSLC22A2 (OCT2) in the cellular uptake of platinum compounds.
  79. Jenkinson S, Chung G, van Loon E, Bakar N, Dalzell A, Brown C. The limitations of renal epithelial cell line HK-2 as a model of drug transporter expression and function in the proximal tubule. Pflugers Arch. 2012;464:601-11 pubmed publisher
    ..qPCR showed no mRNA expression of the SLC22 transporter family (OAT1, OAT3, OCT2) in HK-2 cells compared to renal cortex samples...
  80. Wang Y, Yin J, Li X, Chen J, Qian C, Zheng Y, et al. The association of transporter genes polymorphisms and lung cancer chemotherapy response. PLoS ONE. 2014;9:e91967 pubmed publisher
    ..The main polymorphisms on transporters OCT2, LRP, AQP2, AQP9 and TMEM205 genes were genotyped in 338 lung cancer patients...
  81. Jouan E, Le Vee M, Denizot C, Da Violante G, Fardel O. The mitochondrial fluorescent dye rhodamine 123 is a high-affinity substrate for organic cation transporters (OCTs) 1 and 2. Fundam Clin Pharmacol. 2014;28:65-77 pubmed publisher
    ..to characterize the putative interactions of rhodamine 123 with human organic cation transporter (OCT) 1 and OCT2. Intracellular uptake of the dye was demonstrated to be enhanced in both hOCT1- and hOCT2-overexpressing HEK293 ..
  82. Tong Z, Yerramilli U, Surapaneni S, Kumar G. The interactions of lenalidomide with human uptake and efflux transporters and UDP-glucuronosyltransferase 1A1: lack of potential for drug-drug interactions. Cancer Chemother Pharmacol. 2014;73:869-74 pubmed publisher
    ..proteins (MRP1, MRP2, MRP3), organic anion transporters (OAT1, OAT3), organic cation transporters (OCT1 and OCT2), human organic cation transporter novel 1 and 2 (OCTN1 and OCTN2), multidrug and toxin extrusion (MATE1) and ..
  83. Higashi K, Imamura M, Fudo S, Uemura T, Saiki R, Hoshino T, et al. Identification of functional amino acid residues involved in polyamine and agmatine transport by human organic cation transporter 2. PLoS ONE. 2014;9:e102234 pubmed publisher
    Polyamine (putrescine, spermidine and spermine) and agmatine uptake by the human organic cation transporter 2 (hOCT2) was studied using HEK293 cells transfected with pCMV6-XL4/hOCT2. The Km values for putrescine and spermidine were 7...
  84. Hou W, Zhang D, Lu W, Zheng T, Wan L, Li Q, et al. Polymorphism of organic cation transporter 2 improves glucose-lowering effect of metformin via influencing its pharmacokinetics in Chinese type 2 diabetic patients. Mol Diagn Ther. 2015;19:25-33 pubmed publisher
    This study aimed to investigate how the organic cation transporter 2 nucleotide polymorphism at site 808 (G → T) affects metformin pharmacokinetics and its long-term anti-diabetic effect...
  85. Zaharenko L, Kalnina I, Geldnere K, Konrade I, Grinberga S, Zidzik J, et al. Single nucleotide polymorphisms in the intergenic region between metformin transporter OCT2 and OCT3 coding genes are associated with short-term response to metformin monotherapy in type 2 diabetes mellitus patients. Eur J Endocrinol. 2016;175:531-540 pubmed
    ..response and SNPs rs3119309 and rs7757336 located in the 5' flanking region of the genes coding for Organic cation transporter 2 and rs2481030 located in the 5' flanking region of Organic cation transporter 3 that was supported by ..
  86. Gaudelot K, Gibier J, Pottier N, Hemon B, Van Seuningen I, Glowacki F, et al. Targeting miR-21 decreases expression of multi-drug resistant genes and promotes chemosensitivity of renal carcinoma. Tumour Biol. 2017;39:1010428317707372 pubmed publisher
    ..and dovitinib; (2) decreased expression of multi-drug resistance genes; and (4) increased SLC22A1/OCT1, SLC22A2/OCT2, and SLC31A1/CTR1 platinum influx transporter expression...
  87. Busch A, Karbach U, Miska D, Gorboulev V, Akhoundova A, Volk C, et al. Human neurons express the polyspecific cation transporter hOCT2, which translocates monoamine neurotransmitters, amantadine, and memantine. Mol Pharmacol. 1998;54:342-52 pubmed
    ..However, concentrations of amantadine that are effective for the treatment of Parkinson's disease may increase the interstitial concentrations of dopamine and other aminergic neurotransmitters by competitive inhibition of hOCT2. ..
  88. Lips K, Volk C, Schmitt B, Pfeil U, Arndt P, Miska D, et al. Polyspecific cation transporters mediate luminal release of acetylcholine from bronchial epithelium. Am J Respir Cell Mol Biol. 2005;33:79-88 pubmed
    ..Using immunohistochemistry in rats and humans, OCT1, OCT2, and OCT3 were localized to the luminal membrane of ciliated epithelial cells...
  89. Prasad B, Johnson K, Billington S, Lee C, Chung G, Brown C, et al. Abundance of Drug Transporters in the Human Kidney Cortex as Quantified by Quantitative Targeted Proteomics. Drug Metab Dispos. 2016;44:1920-1924 pubmed
    ..Renal uptake transporters assessed in this study included organic anion transporters (OAT1-OAT4), organic cation transporter 2 (OCT2), organic/carnitine cation transporters (OCTN1 and OCTN2), and sodium-glucose transporter 2 (..
  90. Sprowl J, Ciarimboli G, Lancaster C, Giovinazzo H, Gibson A, Du G, et al. Oxaliplatin-induced neurotoxicity is dependent on the organic cation transporter OCT2. Proc Natl Acad Sci U S A. 2013;110:11199-204 pubmed publisher
    ..We found that the organic cation transporter 2 (OCT2) is expressed on dorsal root ganglia cells within the nervous system where oxaliplatin is known ..
  91. Erman F, Tuzcu M, Orhan C, Sahin N, Sahin K. Effect of lycopene against cisplatin-induced acute renal injury in rats: organic anion and cation transporters evaluation. Biol Trace Elem Res. 2014;158:90-5 pubmed publisher
    ..and the kidney efflux transporters MRP2 and MRP4 levels were significantly increased, whereas OAT1, OAT3, OCT1, and OCT2 levels in kidney were decreased in the treated rats compared with normal control rats...
  92. Gründemann D, Hahne C, Berkels R, Schömig E. Agmatine is efficiently transported by non-neuronal monoamine transporters extraneuronal monoamine transporter (EMT) and organic cation transporter 2 (OCT2). J Pharmacol Exp Ther. 2003;304:810-7 pubmed
    ..In the present study, the non-neuronal monoamine transporters, organic cation transporter (OCT) 1, OCT2, and extraneuronal monoamine transporter (EMT) (gene symbols SLC22A1-A3), both from human and rat, were examined, ..