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MGP002910

UniProt Annotations

Entry Information

Gene Name	solute carrier family 22 (organic cation transporter), member 2
Protein Entry	S22A2_HUMAN
UniProt ID	O15244
Species	Human

Comments

Comment type	Description
Alternative Products	Event=Alternative splicing; Named isoforms=3; Name=1; IsoId=O15244-1; Sequence=Displayed; Name=2; Synonyms=OCT2-A; IsoId=O15244-2; Sequence=VSP_031773, VSP_031774; Name=3; IsoId=O15244-3; Sequence=VSP_031771, VSP_031772; Note=No experimental confirmation available.;
Biophysicochemical Properties	Kinetic parameters: KM=1 mM for agmatine {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=95 uM for amiloride {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=24 uM for ASP {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=34 uM for memantine {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=27 uM for amantadine {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=1.38 mM for metformin {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=1.9 mM for noradrenaline {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=1.9 mM for norepinephrine {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=1.3 mM for histamine {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=0.39 mM for dopamine {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=0.08 mM for serotonine {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=72.6 uM for cimetidine (at pH 7.4 and 37 degrees Celsius) {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=56.1 uM for famotidine {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=65.2 uM for ranitidine {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=431 uM for TEA (isoform 1) {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; KM=63 uM for TEA (isoform 2) {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; Vmax=3770 pmol/min/mg enzyme for TEA uptake (isoform 1) {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; Vmax=314 pmol/min/mg enzyme for TEA uptake (isoform 2) {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; Vmax=11.9 nmol/min/mg enzyme for metformin uptake {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; Vmax=2170 pmol/min/mg enzyme for cimetidine uptake {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; Vmax=204 pmol/min/mg enzyme for famotidine uptake {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576}; Vmax=265 pmol/min/mg enzyme for ranitidine uptake {ECO:0000269\|PubMed:11758759, ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:9687576};
Function	Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, cisplatin and oxaliplatin. 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. {ECO:0000269\|PubMed:12089365, ECO:0000269\|PubMed:12538837, ECO:0000269\|PubMed:15496291, ECO:0000269\|PubMed:15783073, ECO:0000269\|PubMed:16006492, ECO:0000269\|PubMed:16272756, ECO:0000269\|PubMed:16314463, ECO:0000269\|PubMed:16394027, ECO:0000269\|PubMed:16914559, ECO:0000269\|PubMed:16951202, ECO:0000269\|PubMed:17072098, ECO:0000269\|PubMed:17582384, ECO:0000269\|PubMed:9260930, ECO:0000269\|PubMed:9687576}.
Induction	May be down-regulated in diabetic patients. {ECO:0000269\|PubMed:16314463}.
Similarity	Belongs to the major facilitator (TC 2.A.1) superfamily. Organic cation transporter (TC 2.A.1.19) family. {ECO:0000305}.
Subcellular Location	Membrane {ECO:0000305}; Multi-pass membrane protein {ECO:0000305}.
Tissue Specificity	Mainly expressed in kidney. Localized at the luminal membrane and basolateral membrane of kidney distal tubule and proximal tubules. To a lower extent, expressed in neurons of the cerebral cortex and in various subcortical nuclei (at protein levels). Also detected in secretory phase endometrium; in scattered cells in the stroma. {ECO:0000269\|PubMed:11912245, ECO:0000269\|PubMed:17393420, ECO:0000269\|PubMed:9260930, ECO:0000269\|PubMed:9687576}.