ABC pumps and their role in active drug transport.
Pharmacokinetic limitations affect drug bioavailability determining the loss or the reduction of the pharmacological effects. The Gastro Intestinal tract (GI) and the Blood Brain Barrier (BBB) are the most important restrictive and selective physiological lines of defense of the organism. Although several parameters such as LogP, LogD and K(a) have been extensively employed for determining drug bioavailability, the active transports, present in these biological barriers, play an important role for dosing and limiting cell drugs concentration. In particular, ATP Binding Cassette (ABC) transporters are involved in the active transport both in GI and BBB. Their strategic activity and biochemical and pharmacological role are herein treated.
Colabufo
Nicola A
NA
Dipartimento Farmacochimico, Università degli Studi di Bari, Bari, Italy. colabufo@farmchim.uniba.it
Berardi
Francesco
F
Contino
Marialessandra
M
Niso
Mauro
M
Perrone
Roberto
R
D018528:ATP-Binding Cassette Transporters / Q000145:classification / Q000378:metabolism*; D000818:Animals; D001682:Biological Availability; D001693:Biological Transport, Active / Q000502:physiology; D001812:Blood-Brain Barrier / Q000378:metabolism; D015195:Drug Design; D041981:Gastrointestinal Tract / Q000378:metabolism; D006801:Humans; D008954:Models, Biological; D010599:Pharmacokinetics
D018528:ATP-Binding Cassette Transporters