Role of ATP-binding cassette transporters in drug distribution to the heart and protection from toxic compounds

ATP-binding cassette (ABC) transporters consist of a family of proteins that translocate substrates against a concentration gradient from the intracellular toward the extracellular milieu. Among the members of the ABC transporter superfamily, P-glycoprotein has been studied most extensively and has been found to be expressed in tissues such as liver, kidneys, and intestines. This suggests a physiological function for this transporter in the protection and detoxification of the organism. P-glycoprotein and other ABC transporters were also found to be expressed in the myocardium. Current literature suggests that ABC transporters have a role in controlling distribution of xenobiotics to the heart, thus protecting this organ. Heart Metab. 2007;35:1–6.