Skip to content
Licensed Unlicensed Requires Authentication Published by De Gruyter June 18, 2011

Substrate recognition and translocation by polyspecific organic cation transporters

  • Hermann Koepsell EMAIL logo
From the journal Biological Chemistry


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.

Received: 2010-9-14
Accepted: 2010-10-11
Published Online: 2011-06-18
Published in Print: 2011-02-01

©2011 by Walter de Gruyter Berlin New York

Downloaded on 29.9.2023 from
Scroll to top button