01/06/2008 - Reviews
Utilization of membrane vesicle preparations to study drug-ABC transporter interactions
Glavinas H, Méhn D, Jani M, Oosterhuis B, Herédi-Szabó K, Krajcsi P
Expert Opin Drug Metab Toxicol. 2008 Jun;4(6):721-32.
ABSTRACT
BACKGROUND:
The last 15 years have marked an expansion in our understanding of how ABC transporters modulate the pharmacokinetic properties of drugs. Assays based on different membrane preparations were one of the first methods developed to study ABC transporters. Later, they turned out to be valuable tools to gain insight into the nature of drug-ABC transporter interactions.
OBJECTIVES:
Membranes prepared from different sources have been used and characterized; based on the biochemical characteristics of the transport process, a number of different assay types have been developed.
This review focuses on the current experiences on how different membrane-based assays can be utilized in pharmaceutical R&D. Sources of membrane preparations, available assay types and correlation studies between different in-vitro and in-vivo methods are discussed.
Membrane-based assays are valuable tools in drug discovery to characterize drug-ABC transporter interactions.
METHODS: This review focuses on the current experiences on how different membrane-based assays can be utilized in pharmaceutical R&D. Sources of membrane preparations, available assay types and correlation studies between different in-vitro and in-vivo methods are discussed.
RESULTS/CONCLUSION: Membrane-based assays are valuable tools in drug discovery to characterize drug-ABC transporter interactions.
open_in_new Read the Source
Next: Leflunomide and A771726, its metabolite are high affinity substrates of BCRP - implications for drug resistance
Previous: Cholesterol potentiates ABCG2 activity in a heterologous expression system: improved in vitro model to study function of human ABCG2
