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Gene Review

SLC22A2  -  solute carrier family 22 (organic cation...

Homo sapiens

Synonyms: OCT2, Organic cation transporter 2, Solute carrier family 22 member 2, hOCT2
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Disease relevance of SLC22A2

  • It has previously been demonstrated that in cultured and in situ tumour cells of classical Hodgkin lymphoma (cHL), the immunoglobulin (Ig) promoter is inactive and its transcription factors Oct2 and/or BOB.1/OBF.1 are down-regulated [1].
  • Lower Prevalence of the OCT2 Ser270 Allele in Patients with Essential Hypertension* [2].
  • 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 described (Zhang, X., Shirahatti, N. V., Mahadevan, D., and Wright, S. H. (2005) J. Biol. Chem. 280, 34813-34822) [3].

High impact information on SLC22A2

  • Reintroduction of PU.1 and Oct2 in cultured HRS cells restored the activity of cotransduced immunoglobulin enhancer constructs [4].
  • We recently demonstrated that defective immunoglobulin promoter transcription correlates with the down-regulation of the B-cell transcription factors Oct2 and BOB.1/OBF [4].
  • These data demonstrate that cysteine 474 of OCT2 is exposed to the aqueous milieu of the cleft and contributes to forming a pathway for organic cation transport [3].
  • The transport of TEA by hOCT2-A-transfected cells was saturable with the apparent Km value of 63 microM. hOCT2-A stimulated the uptake of TEA, 1-methyl-4-phenylpyridinium, and cimetidine as well as did hOCT2 [5].
  • The uptake of TEA mediated by hOCT2-A but not by hOCT2 was inhibited significantly by organic cations such as procainamide, N-acetylprocainamide, and levofloxacin, indicating that hOCT2-A differs from hOCT2 in its affinity for several compounds [5].

Biological context of SLC22A2

  • The two human organic cation transporter genes SLC22A1 and SLC22A2 are located on chromosome 6q26 [6].
  • Since EMT and OCT2 may play important roles in catecholamine homeostasis and, as such, are candidate genes in human disease, the present results provide a basis for the analysis of genetic variation and the regulation of transcription [7].
  • In contrast, the OCT2 promoter is not associated with a CpG island, contains a putative TATA box, and potential binding sites for specific transcription factors, such as HFH-8 and IK2 [7].
  • From direct DNA sequencing, 7 of 13 coding variants were nonsynonymous single-nucleotide polymorphisms (SNPs), including four variants from hOCT1 (F160L, P283L, P341L, and M408V) and three from hOCT2 (T199I, T201M, and A270S), whereas 6 were synonymous SNPs [8].
  • The functional changes of hOCT2 variants were evaluated in vitro, and those genetic polymorphisms of hOCTs were compared among different ethnic populations [8].

Anatomical context of SLC22A2


Associations of SLC22A2 with chemical compounds

  • However, oxaliplatin showed almost no influence on the TEA uptakes in the HEK293 cells expressing hOCT1, hOCT2, and hOCT3 [14].
  • The contribution of each hOCT was evaluated based on measurements of the intracellular concentrations of haloperidol metabolites in Madin Darby canine kidney (MDCK) cells transfected with hOCT1, hOCT2, or hOCT3 [15].
  • Renal Transport of Adefovir, Cidofovir, and Tenofovir by SLC22A Family Members (hOAT1, hOAT3, and hOCT2) [16].
  • The TEs of OCT1 and OCT2 for dopamine, noradrenaline, adrenaline and 5-HT in general are rather low, in the range relative to MPP+ of 5%-15% [10].
  • This selection may be due to a necessary role of OCT2 in the renal elimination of endogenous amines or xenobiotics, including environmental toxins, neurotoxic amines and therapeutic drugs [17].

Physical interactions of SLC22A2

  • The half-maximal inhibitory concentrations of famotidine for [3H]estrone sulfate transport by hOAT3 and [14C]tetraethylammonium transport by hOCT2 (300 microM and 1.8 mM, respectively) were higher than those of cimetidine (53 and 67 microM, respectively) [18].

Other interactions of SLC22A2

  • The EMT gene is 77 kb, and the OCT2 gene is 45 kb in size [7].
  • SLC22A1 and SLC22A2 localized to the same locus, demonstrating the conservation of the close physical linkage of these three organic cation transporter genes in mouse and human [19].
  • The Ki values of several compounds in interacting with hOCT1 differed substantially from the corresponding values for the rat organic cation transporter, rOCT1, and the human kidney-specific organic cation transporter, hOCT2, determined in previous studies [20].

Analytical, diagnostic and therapeutic context of SLC22A2

  • This study investigated the association of the OCT2 Ala270Ser polymorphism with essential hypertension and its impact on blood pressure status in 607 Caucasian patients who underwent left heart catheterization [2].
  • Inhibition of Ca2+/CaM complex resulted in a significant decrease of Vmax (160-99 photons/s) that can be explained in part by a reduction of the membrane-associated hOCT2 (-22 +/- 6%, n = 9) as determined using FACScan flow cytometry [21].


  1. Differential Emu enhancer activity and expression of BOB.1/OBF.1, Oct2, PU.1, and immunoglobulin in reactive B-cell populations, B-cell non-Hodgkin lymphomas, and Hodgkin lymphomas. Loddenkemper, C., Anagnostopoulos, I., Hummel, M., Jöhrens-Leder, K., Foss, H.D., Jundt, F., Wirth, T., Dörken, B., Stein, H. J. Pathol. (2004) [Pubmed]
  2. Lower Prevalence of the OCT2 Ser270 Allele in Patients with Essential Hypertension*. Lazar, A., Zimmermann, T., Koch, W., Gr??ndemann, D., Sch??mig, A., Kastrati, A., Sch??mig, E. Clin. Exp. Hypertens. (2006) [Pubmed]
  3. Cysteine accessibility in the hydrophilic cleft of human organic cation transporter 2. Pelis, R.M., Zhang, X., Dangprapai, Y., Wright, S.H. J. Biol. Chem. (2006) [Pubmed]
  4. Loss of PU.1 expression is associated with defective immunoglobulin transcription in Hodgkin and Reed-Sternberg cells of classical Hodgkin disease. Jundt, F., Kley, K., Anagnostopoulos, I., Schulze Pröbsting, K., Greiner, A., Mathas, S., Scheidereit, C., Wirth, T., Stein, H., Dörken, B. Blood (2002) [Pubmed]
  5. cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney. Urakami, Y., Akazawa, M., Saito, H., Okuda, M., Inui, K. J. Am. Soc. Nephrol. (2002) [Pubmed]
  6. The two human organic cation transporter genes SLC22A1 and SLC22A2 are located on chromosome 6q26. Koehler, M.R., Wissinger, B., Gorboulev, V., Koepsell, H., Schmid, M. Cytogenet. Cell Genet. (1997) [Pubmed]
  7. Gene structures of the human non-neuronal monoamine transporters EMT and OCT2. Gründemann, D., Schömig, E. Hum. Genet. (2000) [Pubmed]
  8. Identification and functional characterization of genetic variants of human organic cation transporters in a korean population. Kang, H.J., Song, I.S., Shin, H.J., Kim, W.Y., Lee, C.H., Shim, J.C., Zhou, H.H., Lee, S.S., Shin, J.G. Drug Metab. Dispos. (2007) [Pubmed]
  9. Cloning and characterization of two human polyspecific organic cation transporters. Gorboulev, V., Ulzheimer, J.C., Akhoundova, A., Ulzheimer-Teuber, I., Karbach, U., Quester, S., Baumann, C., Lang, F., Busch, A.E., Koepsell, H. DNA Cell Biol. (1997) [Pubmed]
  10. Extraneuronal monoamine transporter and organic cation transporters 1 and 2: A review of transport efficiency. Schömig, E., Lazar, A., Gründemann, D. Handbook of experimental pharmacology. (2006) [Pubmed]
  11. Differential pharmacological in vitro properties of organic cation transporters and regional distribution in rat brain. Amphoux, A., Vialou, V., Drescher, E., Brüss, M., Mannoury La Cour, C., Rochat, C., Millan, M.J., Giros, B., Bönisch, H., Gautron, S. Neuropharmacology (2006) [Pubmed]
  12. Corticosterone-sensitive monoamine transport in the rat dorsomedial hypothalamus: potential role for organic cation transporter 3 in stress-induced modulation of monoaminergic neurotransmission. Gasser, P.J., Lowry, C.A., Orchinik, M. J. Neurosci. (2006) [Pubmed]
  13. Baseline optical coherence tomography predicts the development of glaucomatous change in glaucoma suspects. Lalezary, M., Medeiros, F.A., Weinreb, R.N., Bowd, C., Sample, P.A., Tavares, I.M., Tafreshi, A., Zangwill, L.M. Am. J. Ophthalmol. (2006) [Pubmed]
  14. Cisplatin and Oxaliplatin, but Not Carboplatin and Nedaplatin, Are Substrates for Human Organic Cation Transporters (SLC22A1-3 and Multidrug and Toxin Extrusion Family). Yonezawa, A., Masuda, S., Yokoo, S., Katsura, T., Inui, K. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
  15. Neurotoxic pyridinium metabolites of haloperidol are substrates of human organic cation transporters. Kang, H.J., Lee, S.S., Lee, C.H., Shim, J.C., Shin, H.J., Liu, K.H., Yoo, M.A., Shin, J.G. Drug Metab. Dispos. (2006) [Pubmed]
  16. Renal Transport of Adefovir, Cidofovir, and Tenofovir by SLC22A Family Members (hOAT1, hOAT3, and hOCT2). Uwai, Y., Ida, H., Tsuji, Y., Katsura, T., Inui, K. Pharm. Res. (2007) [Pubmed]
  17. Polymorphisms in a human kidney xenobiotic transporter, OCT2, exhibit altered function. Leabman, M.K., Huang, C.C., Kawamoto, M., Johns, S.J., Stryke, D., Ferrin, T.E., DeYoung, J., Taylor, T., Clark, A.G., Herskowitz, I., Giacomini, K.M. Pharmacogenetics (2002) [Pubmed]
  18. Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A). Motohashi, H., Uwai, Y., Hiramoto, K., Okuda, M., Inui, K. Eur. J. Pharmacol. (2004) [Pubmed]
  19. 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. Verhaagh, S., Schweifer, N., Barlow, D.P., Zwart, R. Genomics (1999) [Pubmed]
  20. Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). Zhang, L., Schaner, M.E., Giacomini, K.M. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  21. 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) [Pubmed]
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