Substrate recognition and translocation by polyspecific organic cation transporters |
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Authors: | Koepsell Hermann |
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Institution: | Institute of Anatomy and Cell Biology, University of Würzburg, Koellikerstrasse 6, Würzburg, Germany. |
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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. |
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