| Identification |
|---|
| HMDB Protein ID
| HMDBP13352 |
| Secondary Accession Numbers
| None |
| Name
| Solute carrier family 22 member 2 |
| Synonyms
|
- Organic cation transporter 2
- rOCT2
|
| Gene Name
| SLC22A2 |
| Protein Type
| Unknown |
| Biological Properties |
|---|
| General Function
| Not Available |
| Specific Function
| Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, serotonin, choline, ranitidine, histamine, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP and amiloride (By similarity). Mediates the influx of adrenaline, noradrenaline (norepinephrine), dopamine, cimetidine, famotidine, metformin, N-1-methylnicotinamide (NMN), 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), oxaliplatin and cisplatin. Cisplatin may develop a nephrotoxic action. Transport of creatinine is inhibited by fluoroquinolones such as DX-619 and LVFX. This transporter is a major determinant of the anticancer activity of oxaliplatin and may contribute to antitumor specificity. |
| Pathways
|
- Choline metabolism in cancer
|
| Reactions
| Not Available |
| GO Classification
|
| Biological Process |
| toxin transport |
| xenobiotic transport |
| quaternary ammonium group transport |
| organic cation transport |
| norepinephrine uptake |
| L-arginine import across plasma membrane |
| L-alpha-amino acid transmembrane transport |
| histamine uptake |
| histamine transport |
| dopamine uptake |
| choline transport |
| amino acid import across plasma membrane |
| xenobiotic transport across blood-brain barrier |
| export across plasma membrane |
| neurotransmitter transport |
| amine transport |
| activation of cysteine-type endopeptidase activity involved in apoptotic process |
| positive regulation of gene expression |
| cation transport |
| serotonin uptake |
| Cellular Component |
| integral to plasma membrane |
| presynapse |
| plasma membrane |
| apical plasma membrane |
| basolateral plasma membrane |
| Molecular Function |
| quaternary ammonium group transmembrane transporter activity |
| steroid binding |
| choline transmembrane transporter activity |
| xenobiotic transporter activity |
| efflux transmembrane transporter activity |
| toxin transporter activity |
| pyrimidine nucleoside transmembrane transporter activity |
| organic cation transmembrane transporter activity |
| monoamine transmembrane transporter activity |
| L-arginine transmembrane transporter activity |
| L-amino acid transmembrane transporter activity |
| amine transmembrane transporter activity |
| neurotransmitter transporter activity |
|
| Cellular Location
|
Not Available
|
| Gene Properties |
|---|
| Chromosome Location
| Not Available |
| Locus
| Not Available |
| SNPs
| Not Available |
| Gene Sequence
|
Not Available
|
| Protein Properties |
|---|
| Number of Residues
| 555 |
| Molecular Weight
| 62341.91 |
| Theoretical pI
| 7.693 |
| Pfam Domain Function
|
|
| Signals
|
Not Available
|
|
Transmembrane Regions
|
- 22-42;151-171;178-198;211-231;239-259;264-284;349-369;376-396;405-425;433-453;465-485;495-515;
|
| Protein Sequence
|
Not Available
|
| External Links |
|---|
| GenBank ID Protein
| Not Available |
| UniProtKB/Swiss-Prot ID
| Q9R0W2 |
| UniProtKB/Swiss-Prot Entry Name
| S22A2_RAT |
| PDB IDs
|
Not Available |
| GenBank Gene ID
| Not Available |
| GeneCard ID
| Not Available |
| GenAtlas ID
| Not Available |
| HGNC ID
| Not Available |
| References |
|---|
| General References
| - Gorboulev V, Ulzheimer JC, Akhoundova A, Ulzheimer-Teuber I, Karbach U, Quester S, Baumann C, Lang F, Busch AE, Koepsell H: Cloning and characterization of two human polyspecific organic cation transporters. DNA Cell Biol. 1997 Jul;16(7):871-81. [PubMed:9260930 ]
- Kimura N, Masuda S, Tanihara Y, Ueo H, Okuda M, Katsura T, Inui K: Metformin is a superior substrate for renal organic cation transporter OCT2 rather than hepatic OCT1. Drug Metab Pharmacokinet. 2005 Oct;20(5):379-86. [PubMed:16272756 ]
- Tahara H, Kusuhara H, Endou H, Koepsell H, Imaoka T, Fuse E, Sugiyama Y: A species difference in the transport activities of H2 receptor antagonists by rat and human renal organic anion and cation transporters. J Pharmacol Exp Ther. 2005 Oct;315(1):337-45. Epub 2005 Jul 8. [PubMed:16006492 ]
- Yokoo S, Yonezawa A, Masuda S, Fukatsu A, Katsura T, Inui K: Differential contribution of organic cation transporters, OCT2 and MATE1, in platinum agent-induced nephrotoxicity. Biochem Pharmacol. 2007 Aug 1;74(3):477-87. Epub 2007 Mar 12. [PubMed:17582384 ]
- Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. [PubMed:10385678 ]
- Grundemann D, Koster S, Kiefer N, Breidert T, Engelhardt M, Spitzenberger F, Obermuller N, Schomig E: Transport of monoamine transmitters by the organic cation transporter type 2, OCT2. J Biol Chem. 1998 Nov 20;273(47):30915-20. [PubMed:9812985 ]
- Okuda M, Saito H, Urakami Y, Takano M, Inui K: cDNA cloning and functional expression of a novel rat kidney organic cation transporter, OCT2. Biochem Biophys Res Commun. 1996 Jul 16;224(2):500-7. doi: 10.1006/bbrc.1996.1056. [PubMed:8702418 ]
- Urakami Y, Okuda M, Saito H, Inui K: Hormonal regulation of organic cation transporter OCT2 expression in rat kidney. FEBS Lett. 2000 May 12;473(2):173-6. doi: 10.1016/s0014-5793(00)01525-8. [PubMed:10812069 ]
- Sugawara-Yokoo M, Urakami Y, Koyama H, Fujikura K, Masuda S, Saito H, Naruse T, Inui K, Takata K: Differential localization of organic cation transporters rOCT1 and rOCT2 in the basolateral membrane of rat kidney proximal tubules. Histochem Cell Biol. 2000 Sep;114(3):175-80. doi: 10.1007/s004180000186. [PubMed:11083459 ]
- Yonezawa A, Masuda S, Nishihara K, Yano I, Katsura T, Inui K: Association between tubular toxicity of cisplatin and expression of organic cation transporter rOCT2 (Slc22a2) in the rat. Biochem Pharmacol. 2005 Dec 5;70(12):1823-31. doi: 10.1016/j.bcp.2005.09.020. Epub 2005 Oct 20. [PubMed:16242669 ]
- Sturm A, Gorboulev V, Gorbunov D, Keller T, Volk C, Schmitt BM, Schlachtbauer P, Ciarimboli G, Koepsell H: Identification of cysteines in rat organic cation transporters rOCT1 (C322, C451) and rOCT2 (C451) critical for transport activity and substrate affinity. Am J Physiol Renal Physiol. 2007 Sep;293(3):F767-79. doi: 10.1152/ajprenal.00106.2007. Epub 2007 Jun 13. [PubMed:17567940 ]
- Matsuzaki T, Morisaki T, Sugimoto W, Yokoo K, Sato D, Nonoguchi H, Tomita K, Terada T, Inui K, Hamada A, Saito H: Altered pharmacokinetics of cationic drugs caused by down-regulation of renal rat organic cation transporter 2 (Slc22a2) and rat multidrug and toxin extrusion 1 (Slc47a1) in ischemia/reperfusion-induced acute kidney injury. Drug Metab Dispos. 2008 Apr;36(4):649-54. doi: 10.1124/dmd.107.019869. Epub 2008 Jan 7. [PubMed:18180268 ]
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