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

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

Research output: Contribution to journalReview article

47 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)47-56
Number of pages10
JournalAdvanced Drug Delivery Reviews
Volume61
Issue number1
DOIs
Publication statusPublished - Jan 31 2009

Keywords

  • ABCG2
  • ADME-Tox
  • Cellular assays
  • Conformation sensitive antibody
  • Fluorescent proteins
  • Membrane-based assays
  • Multidrug resistance

ASJC Scopus subject areas

  • Pharmaceutical Science

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