SLC22A1
entrez
6580
canonical
uniprot
O15245
canonical
ensembl
ENSG00000175003
resolver
ensp
ENSP00000318103
resolver
ensp
ENSP00000355930
resolver
ensp
ENSP00000409557
resolver
ensp
ENSP00000645871
resolver
genesymbol
SLC22A1
resolver
genesymbol_syn
OCT1
resolver
hgnc
HGNC:10963
resolver
uniprot
A6NFF3
resolver
uniprot
A8K1H2
resolver
uniprot
C9JSU6
resolver
uniprot
O15395
resolver
uniprot
Q9NQD4
resolver
uniprot_entry
S22A1_HUMAN
resolver
uniprot_sec
A6NFF3
resolver
uniprot_sec
A8K1H2
resolver
uniprot_sec
C9JSU6
resolver
uniprot_sec
O15395
resolver
uniprot_sec
Q9NQD4
resolver
activity_regulation
ACTIVITY REGULATION: 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). {ECO:0000250|UniProtKB:Q63089, ECO:0000269|PubMed:15389554}.
uniprot
proteins
amino_acid_sequence
MPTVDDILEQVGESGWFQKQAFLILCLLSAAFAPICVGIVFLGFTPDHHCQSPGVAELSQRCGWSPAEELNYTVPGLGPAGEAFLGQCRRYEVDWNQSALSCVDPLASLATNRSHLPLGPCQDGWVYDTPGSSIVTEFNLVCADSWKLDLFQSCLNAGFLFGSLGVGYFADRFGRKLCLLGTVLVNAVSGVLMAFSPNYMSMLLFRLLQGLVSKGNWMAGYTLITEFVGSGSRRTVAIMYQMAFTVGLVALTGLAYALPHWRWLQLAVSLPTFLFLLYYWCVPESPRWLLSQKRNTEAIKIMDHIAQKNGKLPPADLKMLSLEEDVTEKLSPSFADLFRTPRLRKRTFILMYLWFTDSVLYQGLILHMGATSGNLYLDFLYSALVEIPGAFIALITIDRVGRIYPMAMSNLLAGAACLVMIFISPDLHWLNIIIMCVGRMGITIAIQMICLVNAELYPTFVRNLGVMVCSSLCDIGGIITPFIVFRLREVWQALPLILFAVLGLLAAGVTLLLPETKGVALPETMKDAENLGRKAKPKENTIYLKVQTSEPSGT
uniprot
proteins
function
FUNCTION: 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). {ECO:0000250|UniProtKB:O08966, ECO:0000250|UniProtKB:Q63089, ECO:0000269|PubMed:11388889, ECO:0000269|PubMed:11408531, ECO:0000269|PubMed:11907186, ECO:0000269|PubMed:12439218, ECO:0000269|PubMed:12719534, ECO:0000269|PubMed:15389554, ECO:0000269|PubMed:15817714, ECO:0000269|PubMed:16263091, ECO:0000269|PubMed:16272756, ECO:0000269|PubMed:16581093, ECO:0000269|PubMed:17460754, ECO:0000269|PubMed:19536068, ECO:0000269|PubMed:21128598, ECO:0000269|PubMed:23680637, ECO:0000269|PubMed:24961373, ECO:0000269|PubMed:34040533, ECO:0000269|PubMed:35469921, ECO:0000269|PubMed:40972734, ECO:0000269|PubMed:9187257, ECO:0000269|PubMed:9260930, ECO:0000269|PubMed:9655880, ECO:0000305|PubMed:35307651}.; FUNCTION: [Isoform 1]: Mediates the uptake of 1-methyl-4-phenylpyridinium (MPP(+)). {ECO:0000269|PubMed:11388889}.; FUNCTION: [Isoform 2]: Not able to uptake 1-methyl-4-phenylpyridinium (MPP(+)). {ECO:0000269|PubMed:11388889}.; FUNCTION: [Isoform 3]: Not able to uptake 1-methyl-4-phenylpyridinium (MPP(+)). {ECO:0000269|PubMed:11388889}.; FUNCTION: [Isoform 4]: Not able to uptake 1-methyl-4-phenylpyridinium (MPP(+)). {ECO:0000269|PubMed:11388889}.
uniprot
proteins
mass_dalton
61154
uniprot
proteins
mutagenesis
MUTAGEN 24; /note="I->L: No change in fenoterol uptake. No change in trospium uptake. No change in terbutaline uptake."; /evidence="ECO:0000269|PubMed:35469921"; MUTAGEN 28; /note="L->I: No change in fenoterol uptake. No change in trospium uptake. No change in terbutaline uptake."; /evidence="ECO:0000269|PubMed:35469921"; MUTAGEN 31; /note="A->S: No change in fenoterol uptake. No change in trospium uptake. No change in terbutaline uptake."; /evidence="ECO:0000269|PubMed:35469921"; MUTAGEN 32; /note="F->L: No change in fenoterol uptake. Decreased trospium uptake. Decreased trospium affinity."; /evidence="ECO:0000269|PubMed:35469921"; MUTAGEN 36; /note="C->Y: Increased fenoterol uptake. Increased fenoterol affinity. No change in trospium uptake. No change in terbutaline uptake. No change in terbutaline affinity."; /evidence="ECO:0000269|PubMed:35469921"; MUTAGEN 240; /note="Y->F: Decreased TEA uptake."; /evidence="ECO:0000269|PubMed:26979622"; MUTAGEN 283; /note="P->A: Decreased TEA uptake."; /evidence="ECO:0000269|PubMed:26979622"; MUTAGEN 361; /note="Y->F: Decreased TEA uptake."; /evidence="ECO:0000269|PubMed:26979622"; MUTAGEN 376; /note="Y->F: Decreased TEA uptake."; /evidence="ECO:0000269|PubMed:26979622"; MUTAGEN 465; /note="G->A: No changes in MPP(+) uptake."; /evidence="ECO:0000269|PubMed:12719534
uniprot
proteins
post_translational_modification
PTM: Phosphorylated. {ECO:0000250|UniProtKB:Q63089}.
uniprot
proteins
protein_family
Major facilitator (TC 2.A.1) superfamily
uniprot
proteins
protein_family
Organic cation transporter (TC 2.A.1.19) family
uniprot
proteins
pubmed
11388889
uniprot
proteins
pubmed
11408531
uniprot
proteins
pubmed
11907186
uniprot
proteins
pubmed
12439218
uniprot
proteins
pubmed
12719534
uniprot
proteins
pubmed
14574404
uniprot
proteins
pubmed
14697261
uniprot
proteins
pubmed
14702039
uniprot
proteins
pubmed
15389554
uniprot
proteins
pubmed
15489334
uniprot
proteins
pubmed
15499200
uniprot
proteins
pubmed
15817714
uniprot
proteins
pubmed
16263091
uniprot
proteins
pubmed
16272756
uniprot
proteins
pubmed
16436500
uniprot
proteins
pubmed
16581093
uniprot
proteins
pubmed
16914559
uniprot
proteins
pubmed
16951202
uniprot
proteins
pubmed
17460754
uniprot
proteins
pubmed
17635184
uniprot
proteins
pubmed
19536068
uniprot
proteins
pubmed
21128598
uniprot
proteins
pubmed
23680637
uniprot
proteins
pubmed
24275569
uniprot
proteins
pubmed
24961373
uniprot
proteins
pubmed
26979622
uniprot
proteins
pubmed
28942964
uniprot
proteins
pubmed
34040533
uniprot
proteins
pubmed
35307651
uniprot
proteins
pubmed
35469921
uniprot
proteins
pubmed
40972734
uniprot
proteins
pubmed
9187257
uniprot
proteins
pubmed
9260930
uniprot
proteins
pubmed
9655880
uniprot
proteins
sequence_length
554
uniprot
proteins
subcellular_location
SUBCELLULAR LOCATION: Basolateral cell membrane {ECO:0000269|PubMed:12719534}; Multi-pass membrane protein {ECO:0000305}. Apical cell membrane {ECO:0000269|PubMed:15817714, ECO:0000269|PubMed:19536068, ECO:0000269|PubMed:23680637}; Multi-pass membrane protein {ECO:0000305}. Lateral cell membrane {ECO:0000269|PubMed:16263091}; Multi-pass membrane protein {ECO:0000305}. Basal cell membrane {ECO:0000269|PubMed:35307651}; Multi-pass membrane protein {ECO:0000305}. Cell membrane {ECO:0000269|PubMed:35469921}; Multi-pass membrane protein {ECO:0000305}. Note=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). {ECO:0000250|UniProtKB:Q63089, ECO:0000269|PubMed:15817714, ECO:0000269|PubMed:16263091, ECO:0000269|PubMed:19536068, ECO:0000269|PubMed:23680637, ECO:0000269|PubMed:35307651}.
uniprot
proteins
transmembrane_region
TRANSMEM 22..42; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 150..170; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 177..197; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 207..229; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 236..256; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 263..283; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 348..368; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 377..397; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 403..423; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 432..452; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 465..485; /note="Helical"; /evidence="ECO:0000255"; TRANSMEM 493..513; /note="Helical"; /evidence="ECO:0000255
uniprot
proteins