Polyspecific organic cation transporters and their impact on drug intracellular levels and pharmacodynamics.

ABSTRACT: Most drugs are intended to act on molecular targets residing within a specific tissue or cell type. Therefore, the drug concentration within the target tissue or cells is most relevant to its pharmacological effect. Increasing evidences suggest that drug transporters not only play a significant role in governing systemic drug levels, but are also an important gate keeper for intra-tissue and intracellular drug concentrations. This review focuses on polyspecific organic cation transporters, which include the organic cation transporters 1-3 (OCT1-3), the multidrug and toxin extrusion proteins 1-2 (MATE1-2) and the plasma membrane monoamine transporter (PMAT). Following an overview of the tissue distribution, transport mechanisms, and functional characteristics of these transporters, we highl

SUBMITTER: Wagner DJ 

PROVIDER: S-EPMC5293005 | biostudies-literature | 2016 Sep

REPOSITORIES: biostudies-literature