期刊
BIOLOGICAL CHEMISTRY
卷 392, 期 1-2, 页码 95-101出版社
WALTER DE GRUYTER & CO
DOI: 10.1515/BC.2011.009
关键词
organic cation transporters; polyspecific transporters; substrate recognition; transport mechanism
资金
- Deutsche Forschungsgemeinschaft [SFB487/A4]
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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