Antibody binding shift assay for rapid screening of drug interactions with the human ABCG2 multidrug transporter

Ágnes Telbisz, Csilla Hegedüs, Csilla Özvegy-Laczka, Katalin Goda, György Várady, Zoltán Takáts, Eszter Szabó, Brian P. Sorrentino, András Váradi, Balázs Sarkadi

Research output: Contribution to journalArticle

17 Citations (Scopus)


The ABCG2 multidrug transporter protein has been identified as a key player in cancer drug resistance and xenobiotic elimination, as its actively transported substrates include anticancer drugs, intermediates of heme metabolism, xenobiotics, and also drug conjugates. Several transported substrates at higher concentrations, and some anticancer agents even at low concentrations directly inhibit the ABCG2 transporter, thus it is difficult to provide estimation for pharmacologically important ABCG2-dependent interactions. In addition, as documented here, in mutant variants of the transporter, inhibitors of the wild-type ABCG2 may become actively transported substrates. In this paper we describe a rapid in vitro assay to identify transport modulation by measuring the cell surface interaction of a conformation sensitive monoclonal antibody (5D3) with ABCG2 in intact cells. As documented, in conjunction with membrane ATPase, transport and cytotoxicity measurements, this assay provides a reliable estimate of concentration-dependent modulation of ABCG2 by newly emerging pharmacophores. A high-throughput, 96-well plate assay platform is also provided.

Original languageEnglish
Pages (from-to)101-109
Number of pages9
JournalEuropean Journal of Pharmaceutical Sciences
Issue number1-2
Publication statusPublished - Jan 23 2012


  • Anti-ABCG2 monoclonal antibody
  • Drug interactions with ABCG2
  • High-throughput antibody shift assay
  • Human ABCG2 multidrug transporter
  • Inhibitors of ABCG2

ASJC Scopus subject areas

  • Pharmaceutical Science

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