Uptake transporters of the human OATP family: molecular characteristics, substrates, their role in drug-drug interactions, and functional consequences of polymorphisms.
Article Details
- CitationCopy to clipboard
Konig J
Uptake transporters of the human OATP family: molecular characteristics, substrates, their role in drug-drug interactions, and functional consequences of polymorphisms.
Handb Exp Pharmacol. 2011;(201):1-28. doi: 10.1007/978-3-642-14541-4_1.
- PubMed ID
- 21103967 [ View in PubMed]
- Abstract
Organic anion transporting polypeptides (OATPs, gene family: SLC21/SLCO) mediate the uptake of a broad range of substrates including several widely prescribed drugs into cells. Drug substrates for members of the human OATP family include HMG-CoA-reductase inhibitors (statins), antibiotics, anticancer agents, and cardiac glycosides. OATPs are expressed in a variety of different tissues including brain, intestine, liver, and kidney, suggesting that these uptake transporters are important for drug absorption, distribution, and excretion. Because of their wide tissue distribution and broad substrate spectrum, altered transport kinetics, for example, due to drug-drug interactions or due to the functional consequences of genetic variations (polymorphisms), can contribute to the interindividual variability of drug effects. Therefore, the molecular characteristics of human OATP family members, the role of human OATPs in drug-drug interactions, and the in vitro analysis of the functional consequences of genetic variations in SLCO genes encoding OATP proteins are the focus of this chapter.
DrugBank Data that Cites this Article
- Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Erythromycin Solute carrier organic anion transporter family member 1B1 Protein Humans NoSubstrateInhibitorDetails Erythromycin Solute carrier organic anion transporter family member 1B3 Protein Humans UnknownSubstrateInhibitorDetails Telithromycin Solute carrier organic anion transporter family member 1B1 Protein Humans UnknownInhibitorDetails Telithromycin Solute carrier organic anion transporter family member 1B3 Protein Humans UnknownInhibitorDetails