Protein name: OCT1 Aliases: N/D Substrates: organic cations Transport type: Facilitated transporter Tissue and cellular expression: liver, small intestine, kidney, lung, skeletal muscle, brain (endothelial cells of blood-brain barrier), adipose tissue, immune cells Subcellular expression: sinusoidal membrane of hepatocytes (liver) Disease: cytotoxicity of oxaliplatin and picoplatin Locus: 6q26 Sequence ID: NP_003048.1, NM_003057.2 NP_694857.1, NM_153187.1 Gene ID: 6580 Splice variants: 3 splice variants from liver with no uptake in vitro

S22A1_HUMAN (UniProt)

Gene names: SLC22A1, OCT1
Protein names and data: S22A1_HUMAN, Full=Solute carrier family 22 member 1, Full=Organic cation transporter 1;Short=hOCT1; Length: 554 a.a., Mass: 61154 Da,
fasta formatted sequence

Function: Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)- N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine, and metformin. The transport of organic cations is inhibited by a broad array of compounds like tetramethylammonium (TMA), cocaine, lidocaine, NMDA receptor antagonists, atropine, prazosin, cimetidine, TEA and NMN, guanidine, cimetidine, choline, procainamide, quinine, tetrabutylammonium, and tetrapentylammonium. Translocates organic cations in an electrogenic and pH-independent manner. Translocates organic cations across the plasma membrane in both directions. Transports the polyamines spermine and spermidine. Transports pramipexole across the basolateral membrane of the proximal tubular epithelial cells. The choline transport is activated by MMTS. Regulated by various intracellular signaling pathways including inhibition by protein kinase A activation, and endogenously activation by the calmodulin complex, the calmodulin- dependent kinase II and LCK tyrosine kinase
Cellular location: Basolateral cell membrane; Multi-pass membrane protein
Tissue specificity: Widely expressed with high level in liver. Isoform 1 and isoform 2 are expressed in liver. Isoform 1, isoform 2, isoform 3 and isoform 4 are expressed in glial cell lines

Database cross-references

UniProt: O15245
NextBio: 25603
OMIM: 602607
Ensembl: ENST00000460902
GeneCard: GC06P160121
PharmGenUCSF: SLC22A1
Guide to Pharmacology: SLC22A1 (1019)
Organic cation transporters (OCT) (1019)

HGNC: HGNC:10963

Genetic variants

See also Ensembl:ENST00000460902