Abstract
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 Ka 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.
Keywords: Blood brain barrier, ABC transporters, P-glycoprotein, MRPs, drug absorption and disposition
Current Topics in Medicinal Chemistry
Title: ABC Pumps and Their Role in Active Drug Transport
Volume: 9 Issue: 2
Author(s): Nicola A. Colabufo, Francesco Berardi, Marialessandra Contino, Mauro Niso and Roberto Perrone
Affiliation:
Keywords: Blood brain barrier, ABC transporters, P-glycoprotein, MRPs, drug absorption and disposition
Abstract: 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 Ka 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.
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Cite this article as:
Colabufo A. Nicola, Berardi Francesco, Contino Marialessandra, Niso Mauro and Perrone Roberto, ABC Pumps and Their Role in Active Drug Transport, Current Topics in Medicinal Chemistry 2009; 9 (2) . https://dx.doi.org/10.2174/156802609787521553
DOI https://dx.doi.org/10.2174/156802609787521553 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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