{"entryType":"UniProtKB reviewed (Swiss-Prot)","primaryAccession":"O15245","secondaryAccessions":["A6NFF3","A8K1H2","C9JSU6","O15395","Q9NQD4"],"uniProtkbId":"S22A1_HUMAN","entryAudit":{"firstPublicDate":"2008-05-20","lastAnnotationUpdateDate":"2026-09-02","lastSequenceUpdateDate":"2010-11-30","entryVersion":196,"sequenceVersion":2},"annotationScore":5.0,"organism":{"scientificName":"Homo sapiens","commonName":"Human","taxonId":9606,"lineage":["Eukaryota","Metazoa","Chordata","Craniata","Vertebrata","Euteleostomi","Mammalia","Eutheria","Euarchontoglires","Primates","Haplorrhini","Catarrhini","Hominidae","Homo"]},"proteinExistence":"1: Evidence at protein level","proteinDescription":{"recommendedName":{"fullName":{"evidences":[{"evidenceCode":"ECO:0000303","source":"PubMed","id":"11388889"}],"value":"Solute carrier family 22 member 1"}},"alternativeNames":[{"fullName":{"evidences":[{"evidenceCode":"ECO:0000303","source":"PubMed","id":"9260930"}],"value":"Organic cation transporter 1"},"shortNames":[{"evidences":[{"evidenceCode":"ECO:0000303","source":"PubMed","id":"9260930"}],"value":"hOCT1"}]}]},"genes":[{"geneName":{"evidences":[{"evidenceCode":"ECO:0000312","source":"HGNC","id":"HGNC:10963"}],"value":"SLC22A1"},"synonyms":[{"value":"OCT1"}]}],"comments":[{"texts":[{"evidences":[{"evidenceCode":"ECO:0000250","source":"UniProtKB","id":"O08966"},{"evidenceCode":"ECO:0000250","source":"UniProtKB","id":"Q63089"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11408531"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11907186"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"12439218"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"12719534"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"15389554"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"15817714"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16263091"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16272756"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16581093"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"17460754"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"19536068"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"21128598"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"23680637"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"24961373"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"34040533"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"40972734"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"9187257"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"9260930"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"9655880"},{"evidenceCode":"ECO:0000305","source":"PubMed","id":"35307651"}],"value":"Electrogenic voltage-dependent uniporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:11388889, PubMed:11408531, PubMed:12439218, PubMed:12719534, PubMed:15389554, PubMed:16263091, PubMed:16272756, PubMed:16581093, PubMed:19536068, PubMed:21128598, PubMed:23680637, PubMed:24961373, PubMed:34040533, PubMed:9187257, PubMed:9260930, PubMed:9655880). Functions as a pH- and Na(+)-independent, bidirectional transporter (By similarity). Cation cellular uptake or release is driven by the electrochemical potential (i.e. membrane potential and concentration gradient) and substrate selectivity (By similarity). Hydrophobicity is a major requirement for recognition in polyvalent substrates and inhibitors (By similarity). Primarily expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (By similarity). Most likely functions as an uptake carrier in enterocytes contributing to the intestinal elimination of organic cations from the systemic circulation (PubMed:16263091). Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline (PubMed:12439218, PubMed:24961373, PubMed:35469921, PubMed:9260930). Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover (PubMed:21128598). Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism (PubMed:24961373). Also transport choline, albeit with low affinity (PubMed:40972734). Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium (PubMed:15817714). Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficiency (PubMed:17460754). Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). May contribute to the transport of cationic compounds in testes across the blood-testis-barrier (Probable). Also involved in the uptake of xenobiotics tributylmethylammonium (TBuMA), quinidine, N-methyl-quinine (NMQ), N-methyl-quinidine (NMQD) N-(4,4-azo-n-pentyl)-quinuclidine (APQ), azidoprocainamide methoiodide (AMP), N-(4,4-azo-n-pentyl)-21-deoxyajmalinium (APDA) and 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:11408531, PubMed:15389554, PubMed:35469921, PubMed:9260930)"}],"commentType":"FUNCTION"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"}],"value":"Mediates the uptake of 1-methyl-4-phenylpyridinium (MPP(+))"}],"commentType":"FUNCTION","molecule":"Isoform 1"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"}],"value":"Not able to uptake 1-methyl-4-phenylpyridinium (MPP(+))"}],"commentType":"FUNCTION","molecule":"Isoform 2"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"}],"value":"Not able to uptake 1-methyl-4-phenylpyridinium (MPP(+))"}],"commentType":"FUNCTION","molecule":"Isoform 3"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"}],"value":"Not able to uptake 1-methyl-4-phenylpyridinium (MPP(+))"}],"commentType":"FUNCTION","molecule":"Isoform 4"},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"1-methylnicotinamide(out) = 1-methylnicotinamide(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:73859"},{"database":"ChEBI","id":"CHEBI:16797"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"9260930"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"dopamine(out) = dopamine(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:73863"},{"database":"ChEBI","id":"CHEBI:59905"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"serotonin(out) = serotonin(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:73867"},{"database":"ChEBI","id":"CHEBI:350546"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"12439218"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"24961373"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"(R)-adrenaline(out) = (R)-adrenaline(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:73875"},{"database":"ChEBI","id":"CHEBI:71406"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"histamine(out) = histamine(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:73879"},{"database":"ChEBI","id":"CHEBI:58432"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"guanidine(out) = guanidine(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:73883"},{"database":"ChEBI","id":"CHEBI:30087"}],"evidences":[{"evidenceCode":"ECO:0000250","source":"UniProtKB","id":"Q63089"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"acetylcholine(in) = acetylcholine(out)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:74663"},{"database":"ChEBI","id":"CHEBI:15355"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"15817714"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"thiamine(in) = thiamine(out)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:34919"},{"database":"ChEBI","id":"CHEBI:18385"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"24961373"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"agmatine(out) = agmatine(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:72131"},{"database":"ChEBI","id":"CHEBI:58145"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"21128598"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"putrescine(out) = putrescine(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:72135"},{"database":"ChEBI","id":"CHEBI:326268"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"21128598"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"spermidine(in) = spermidine(out)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:35039"},{"database":"ChEBI","id":"CHEBI:57834"}],"evidences":[{"evidenceCode":"ECO:0000250","source":"UniProtKB","id":"Q63089"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"L-histidyl-L-proline diketopiperazine(in) = L-histidyl-L-proline diketopiperazine(out)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:74787"},{"database":"ChEBI","id":"CHEBI:90039"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"17460754"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"(R)-salsolinol(in) = (R)-salsolinol(out)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:74791"},{"database":"ChEBI","id":"CHEBI:194082"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"17460754"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"prostaglandin F2alpha(out) = prostaglandin F2alpha(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:50988"},{"database":"ChEBI","id":"CHEBI:57404"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11907186"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"prostaglandin E2(out) = prostaglandin E2(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:50984"},{"database":"ChEBI","id":"CHEBI:606564"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11907186"}]}},{"commentType":"CATALYTIC ACTIVITY","reaction":{"name":"choline(out) = choline(in)","reactionCrossReferences":[{"database":"Rhea","id":"RHEA:32751"},{"database":"ChEBI","id":"CHEBI:15354"}],"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"40972734"}]}},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000250","source":"UniProtKB","id":"Q63089"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"15389554"}],"value":"Phosphorylation of the transporter leads to changes in its substrate affinity, resulting in a regulation of the transport activity (PubMed:15389554). In contrast with rat ortholog, ASP uptake is inhibited by protein kinase A (PKA) and C (PKC) activation (PubMed:15389554). ASP uptake is also endogenously activated by calmodulin, the calmodulin-dependent kinase II and LCK tyrosine kinase (PubMed:15389554). Inhibited by cGMP, most likely through a cGMP-binding protein that interacts with OCT1 (By similarity)"}],"commentType":"ACTIVITY REGULATION"},{"commentType":"BIOPHYSICOCHEMICAL PROPERTIES","kineticParameters":{"maximumVelocities":[{"velocity":1.0,"unit":"nmol/min/mg","enzyme":"enzyme for salsolinol uptake","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"17460754"}]},{"velocity":1.123,"unit":"nmol/min/mg","enzyme":"enzyme with adrenaline as substrate","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]},{"velocity":6.9,"unit":"nmol/min/mg","enzyme":"enzyme for cyclo(his-pro) uptake","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"17460754"}]},{"velocity":6.183,"unit":"nmol/min/mg","enzyme":"enzyme with serotonin as substrate","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]},{"velocity":0.718,"unit":"nmol/min/mg","enzyme":"enzyme with dopamine as substrate","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]},{"velocity":2.77,"unit":"nmol/min/mg","enzyme":"enzyme with thiamine as substrate","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"24961373"}]},{"velocity":8.261,"unit":"nmol/min/mg","enzyme":"enzyme with thiamine as substrate","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]},{"velocity":5.124,"unit":"nmol/min/mg","enzyme":"enzyme with histamine as substrate","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]},{"velocity":2.891,"unit":"nmol/min/mg","enzyme":"enzyme with choline as substrate","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"40972734"}]}],"michaelisConstants":[{"constant":440.0,"unit":"uM","substrate":"salsolinol","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"17460754"}]},{"constant":558.0,"unit":"uM","substrate":"adrenaline","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]},{"constant":655.0,"unit":"uM","substrate":"cyclo(his-pro)","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"17460754"}]},{"constant":663.0,"unit":"uM","substrate":"serotonin","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]},{"constant":674.0,"unit":"uM","substrate":"dopamine","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]},{"constant":647.0,"unit":"nM","substrate":"prostaglandin E2","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11907186"}]},{"constant":477.0,"unit":"nM","substrate":"prostaglandin F2-alpha","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11907186"}]},{"constant":780.0,"unit":"uM","substrate":"thiamine","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"24961373"}]},{"constant":1057.0,"unit":"uM","substrate":"thiamine","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]},{"constant":4675.0,"unit":"uM","substrate":"histamine","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}]},{"constant":18730.0,"unit":"uM","substrate":"agmatine","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"21128598"}]},{"constant":3445.0,"unit":"uM","substrate":"choline","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"40972734"}]},{"constant":19.5,"unit":"uM","substrate":"NMQ","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11408531"}]},{"constant":11.5,"unit":"uM","substrate":"NMQD","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11408531"}]},{"constant":53.0,"unit":"uM","substrate":"TBuMA","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11408531"}]},{"constant":100.9,"unit":"uM","substrate":"APM","evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11408531"}]}]},"phDependence":{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11408531"}],"value":"Optimum pH is 8.5 for the transport of MPP (PubMed:11388889). While optimum pH is 6.0 for the transport of the drug quinidine, no transport activity is observed at pH 7.5, possibly due to the protonation of quininide at pH6.0 (PubMed:11408531)."}]},"temperatureDependence":{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"9655880"}],"value":"Optimum temperature is 22 degrees Celsius for the transport of TEA. Doesn't show any transport activity of TEA at 4 degrees Celsius."}]}},{"commentType":"INTERACTION","interactions":[{"interactantOne":{"uniProtKBAccession":"O15245","intActId":"EBI-1172714"},"interactantTwo":{"uniProtKBAccession":"Q96G23","geneName":"CERS2","intActId":"EBI-1057080"},"numberOfExperiments":3,"organismDiffer":false},{"interactantOne":{"uniProtKBAccession":"O15245","intActId":"EBI-1172714"},"interactantTwo":{"uniProtKBAccession":"Q9BZL3","geneName":"SMIM3","intActId":"EBI-741850"},"numberOfExperiments":3,"organismDiffer":false}]},{"commentType":"SUBCELLULAR LOCATION","note":{"texts":[{"evidences":[{"evidenceCode":"ECO:0000250","source":"UniProtKB","id":"Q63089"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"15817714"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16263091"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"19536068"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"23680637"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35307651"}],"value":"Localized to the sinusoidal/basolateral membrane of hepatocytes (By similarity). Mainly localized to the basolateral membrane of renal proximal tubular cells (By similarity). However, also identified at the apical side of proximal tubular cells (PubMed:19536068). Mainly expressed at the lateral membrane of enterocytes (PubMed:16263091). Also observed at the apical side of enterocytes (PubMed:23680637). Localized to the luminal/apical membrane of ciliated epithelial cells in bronchi (PubMed:15817714). Localized to the basal membrane of Sertoli cells (PubMed:35307651)"}]},"subcellularLocations":[{"location":{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"12719534"}],"value":"Basolateral cell membrane","id":"SL-0026"},"topology":{"evidences":[{"evidenceCode":"ECO:0000305"}],"value":"Multi-pass membrane protein","id":"SL-9909"}},{"location":{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"15817714"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"19536068"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"23680637"}],"value":"Apical cell membrane","id":"SL-0015"},"topology":{"evidences":[{"evidenceCode":"ECO:0000305"}],"value":"Multi-pass membrane protein","id":"SL-9909"}},{"location":{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16263091"}],"value":"Lateral cell membrane","id":"SL-0153"},"topology":{"evidences":[{"evidenceCode":"ECO:0000305"}],"value":"Multi-pass membrane protein","id":"SL-9909"}},{"location":{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35307651"}],"value":"Basal cell membrane","id":"SL-0024"},"topology":{"evidences":[{"evidenceCode":"ECO:0000305"}],"value":"Multi-pass membrane protein","id":"SL-9909"}},{"location":{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}],"value":"Cell membrane","id":"SL-0039"},"topology":{"evidences":[{"evidenceCode":"ECO:0000305"}],"value":"Multi-pass membrane protein","id":"SL-9909"}}]},{"commentType":"ALTERNATIVE PRODUCTS","events":["Alternative splicing"],"isoforms":[{"name":{"value":"1"},"synonyms":[{"value":"hOCT1G/L554"}],"isoformIds":["O15245-1"],"isoformSequenceStatus":"Displayed"},{"name":{"value":"2"},"synonyms":[{"value":"hOCT1G/L506"}],"isoformIds":["O15245-2"],"sequenceIds":["VSP_033589","VSP_033590"],"isoformSequenceStatus":"Described"},{"name":{"value":"3"},"synonyms":[{"value":"hOCT1G483"}],"isoformIds":["O15245-3"],"sequenceIds":["VSP_033588"],"isoformSequenceStatus":"Described"},{"name":{"value":"4"},"synonyms":[{"value":"hOCT1G353"}],"isoformIds":["O15245-4"],"sequenceIds":["VSP_033587"],"isoformSequenceStatus":"Described"}]},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"15817714"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16263091"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"23680637"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35307651"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"9187257"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"9260930"}],"value":"Widely expressed with high level in liver (PubMed:11388889, PubMed:23680637, PubMed:9187257, PubMed:9260930). In liver, expressed around the central vein (PubMed:16263091). Expressed in kidney (PubMed:9187257, PubMed:9260930). Expressed in small intestine enterocytes (PubMed:16263091, PubMed:23680637). Localized to peritubular myoid cells, Leydig cells and moderately to the basal membrane of Sertoli cells in testes (PubMed:35307651). Expressed in tracheal and bronchial ciliated epithelium in the respiratory tract (PubMed:15817714). Also expressed in skeletal muscle, stomach, spleen, heart, placentacolon, brain, granulycytes and lymphocytes (PubMed:9187257, PubMed:9260930)"}],"commentType":"TISSUE SPECIFICITY"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"}],"value":"Expressed in liver and in glial cell lines"}],"commentType":"TISSUE SPECIFICITY","molecule":"Isoform 1"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"}],"value":"Expressed in liver and in glial cell lines"}],"commentType":"TISSUE SPECIFICITY","molecule":"Isoform 2"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"}],"value":"Expressed in glial cell lines. Not expressed in liver"}],"commentType":"TISSUE SPECIFICITY","molecule":"Isoform 3"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"}],"value":"Expressed in glial cell lines. Not expressed in liver"}],"commentType":"TISSUE SPECIFICITY","molecule":"Isoform 4"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16436500"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"17635184"}],"value":"In the liver activated by HNF4A and suppressed by bile acids via NR0B2. Increased by cholesterol treatment in hepatocyte cells"}],"commentType":"INDUCTION"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000250","source":"UniProtKB","id":"Q63089"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}],"value":"A large substrate binding region with partially overlapping binding domains for structurally different substrates is formed by several transmembrane helix domains (TMH) including TMH 2, 4, 10 and 11, and it is alternatingly exposed to the extracellular or intracellular side during substrate transport (By similarity). Amino acids in TMH 1 confer major functional differences between human and mouse orthologs (PubMed:35469921)"}],"commentType":"DOMAIN"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000305","source":"PubMed","id":"26979622"}],"value":"Contains one proline-rich sequence (Pro-Glu-Ser-Pro-Arg) that is required for transport activity"}],"commentType":"DOMAIN"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000250","source":"UniProtKB","id":"Q63089"}],"value":"Phosphorylated"}],"commentType":"PTM"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000269","source":"PubMed","id":"11388889"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"12439218"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"12719534"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16263091"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16272756"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16581093"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16914559"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16951202"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"19536068"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"23680637"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"24961373"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"34040533"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"9187257"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"9260930"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"9655880"}],"value":"Involved in the uptake of clinically used drugs including diabetes treatment medicine metformin, neurotoxins 1-methyl-4-phenylpyridinium (MPP(+)) and iobenguane and platinum-based drug cisplatin (PubMed:11388889, PubMed:12439218, PubMed:12719534, PubMed:16263091, PubMed:16272756, PubMed:16581093, PubMed:16914559, PubMed:16951202, PubMed:19536068, PubMed:23680637, PubMed:24961373, PubMed:35469921, PubMed:9187257, PubMed:9260930, PubMed:9655880). Also involved in metformin efflux transport (PubMed:34040533). Metformin competitively inhibits OCT1-mediated thiamine uptake, leading to a decrease in hepatic steatosis (PubMed:24961373). Plays a role in the anticancer activity of cisplatin and may contribute to antitumor specificity (PubMed:16914559, PubMed:16951202)"}],"commentType":"MISCELLANEOUS"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000305"}],"value":"May be produced at very low levels due to a premature stop codon in the mRNA, leading to nonsense-mediated mRNA decay"}],"commentType":"MISCELLANEOUS","molecule":"Isoform 4"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000305"}],"value":"Belongs to the major facilitator (TC 2.A.1) superfamily. Organic cation transporter (TC 2.A.1.19) family"}],"commentType":"SIMILARITY"},{"texts":[{"evidences":[{"evidenceCode":"ECO:0000250","source":"UniProtKB","id":"Q63089"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16263091"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"16581093"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"19536068"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"23680637"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"28942964"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"34040533"},{"evidenceCode":"ECO:0000269","source":"PubMed","id":"35469921"}],"value":"Cellular localization of OCT1 in the intestine and the kidney remains to be finally defined. While most authors have deduced a localization at the basolateral side of enterocytes consistent with a physiological role in organic anions uptake from the blood flow and intestinal excretion (PubMed:16263091), other studies demonstrated an apical localization (PubMed:23680637), supporting a function in intestinal absorption of organic anions and drugs (PubMed:16263091, PubMed:23680637). Similarly, contradictory results localized the transporter to the basolateral side (By similarity) or to the apical side (PubMed:19536068) of proximal tubules (By similarity) (PubMed:19536068). Although initially reported to transport carnitine across the hepatocyte membrane (PubMed:28942964), another study was unable to verify this finding (PubMed:28942964, PubMed:34040533). Affinity and capacity of the transporter for endogenous substrates vary among orthologs (PubMed:16581093, PubMed:34040533, PubMed:35469921). For endogenous compounds such as dopamine, histamine, serotonin and thiamine, mouse ortholog display higher affinity and capacity compared with human OCT1 (PubMed:35469921). In contrast with mouse ortholog, not able to transport carnitine, noradrenaline (PubMed:34040533)"}],"commentType":"CAUTION"}],"features":[{"type":"Chain","location":{"start":{"value":1,"modifier":"EXACT"},"end":{"value":554,"modifier":"EXACT"}},"description":"Solute carrier family 22 member 1","featureId":"PRO_0000333875"},{"type":"Topological domain","location":{"start":{"value":1,"modifier":"EXACT"},"end":{"value":21,"modifier":"EXACT"}},"description":"Cytoplasmic","evidences":[{"evidenceCode":"ECO:0000255"}]},{"type":"Transmembrane","location":{"start":{"value":22,"modifier":"EXACT"},"end":{"value":42,"modifier":"EXACT"}},"description":"Helical","evidences":[{"evidenceCode":"ECO:0000255"}]},{"type":"Topological 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