PharmGKB summary

Organic cationic transporter 1 (OCT1, encoded by gene SLC22A1) is one of the three similar polyspecific cationic transporters mediating the uptake of many organic cations from the blood into epithelial cells. SLC22A1 is located in a cluster on chromosome 6 and contains seven exons and six introns. It can produce several alternatively spliced mRNA isoforms [1]. Similar to other members of the SLC22 family, the OCT1 protein contains 12 predicted α-helical transmembrane domains and a long hydrophilic loop between transmembrane domains 1 and 2 [2,3]. OCT1 is one of the major hepatic-uptake transporters located on the sinusoidal membrane of hepatocytes. It has substrate selectivity for a variety of endogenous ligands (dopamine, serotonin, choline), as well as cationic drugs, such as metformin, cimetidine, imatinib, oxaliplatin, tramadol, and agmatine [2,4–8]. This PharmGKB summary discusses SLC22A1 and its pharmacogenomic importance. A fully interactive version of this short review, with links to individual paper annotations can be found at: http://www.pharmgkb.org/gene/PA329#tabview = tab3&subtab = 33.