title: Substrate recognition and translocation by polyspecific organic cation transporters.
abstract: Organic cation transporters (OCTs) of the SLC22 family play a pivotal role in distribution and excretion of cationic drugs. They mediate electrogenic translocation of cations in both directions. OCTs are polyspecific transporters. During substrate translocation they perform a series of conformational changes involving an outward-facing conformation, an occluded state and an inward-facing conformation. Mutagenesis of OCT1 in combination with homology modeling showed that identical amino acids form the innermost parts of the outward-open and inward-open binding clefts. In addition to low affinity substrate binding sites, OCT1 contains high affinity substrate binding sites that can mediate inhibition via non-transported compounds.
authors.affiliation: Institute of Anatomy and Cell Biology, University of Würzburg, Koellikerstrasse 6, Würzburg, Germany.
authors.forename: Hermann
authors.initials: H
authors.lastname: Koepsell
mesh_terms: D001665:Binding Sites; D027701:Organic Cation Transport Proteins / Q000737:chemistry / Q000378:metabolism*; D021381:Protein Transport; D013379:Substrate Specificity
chemical_list: D027701:Organic Cation Transport Proteins