Ins and outs of the ABCG2 multidrug transporter: an update on in vitro functional assays.
The major aim of this chapter is to provide a critical overview of the in vitro methods available for studying the function of the ABCG2 multidrug transporter protein. When describing the most applicable assay systems, in each case we present a short overview relevant to ABC multidrug transporters in general, and then we concentrate on the tools applicable to analysis of substrate-drug interactions, the effects of potential activators and inhibitors, and the role of polymorphisms of the ABCG2 transporter. Throughout this chapter we focus on recently developed assay systems, which may provide new possibilities for analyzing the pharmacological aspects of this medically important protein.
Hegedus
Csilla
C
Membrane Research Group, Hungarian Academy of Sciences, Semmelweis University, and National Blood Center, Budapest, Hungary.
Szakács
Gergely
G
Homolya
László
L
Orbán
Tamás I
TI
Telbisz
Agnes
A
Jani
Márton
M
Sarkadi
Balázs
B
D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000037:antagonists & inhibitors / Q000235:genetics / Q000502:physiology*; D001681:Biological Assay / Q000379:methods*; D004347:Drug Interactions; D018432:Drug Resistance, Multiple / Q000502:physiology*; D006801:Humans; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors / Q000235:genetics / Q000502:physiology*; D013379:Substrate Specificity
C116614:ABCG2 protein, human; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D009363:Neoplasm Proteins