12/12/2009 - Reviews

Ins and outs of the ABCG2 multidrug transporter: An update on in vitro functional assays

Csilla Hegedűs, Gergely Szakács, László Homolya, Tamás I. Orbán, Ágnes Telbisz, Márton Jani and Balázs Sarkadi

Adv Drug Deliv Rev. 2009 Jan 31;61(1):47-56. Epub 2008 Dec 24.


The major aim of this chapter is to provide a critical overview of the in vitromethods 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.

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