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

Substrate recognition and translocation by polyspecific organic cation transporters

Hermann Koepsell
From the journal


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

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