Barrière hémato-encéphalique : implication des transporteurs ABC en neuropharmacologie

ATP-binding cassette (ABC) transporters superfamily consists in transmembrane transport proteins that translocate numerous endogenous compounds and xenobiotics across cell membranes. Some ABC transporters, including the well-known P-glycoprotein, are expressed at the blood-brain barrier where they limit the entry into the brain of their substrates including numerous drugs. Thus, inhibition of the efflux transporters by some drugs can lead to CNS side effects due to drug uptake that are normally pumped back into the blood by those transporters. Moreover, this efflux may be responsible for the pharmacoresistance observed in several brain diseases like epilepsy and brain tumours. The aim of this review is to summarize the characteristics of ABC transporters expressed at the human blood-brain barrier and to focus on pharmacological and clinical relevance of this expression.