ABC Transporters

Members of ABC superfamily use ATP as energy source, which allows them to pump substrates against a concentration gradient. Drugs can be simultaneously substrates or inhibitors of more than one efflux transporter, suggesting that ABC transporters employ a combined role in detoxification at above organs. Furthermore, the simultaneous down-regulation and induction of these transporters can occur following administration of a single compound. Down-regulation or inhibition of ABC efflux transporters can be used as a strategy to improve oral drug bioavailability of known substrates, as these transporters prevent drugmolecules from being absorbed.