PI3-kinase and mTOR inhibitors differently modulate the function of the ABCG2 multidrug transporter

Csilla Hegedüs, Krisztina Truta-Feles, Géza Antalffy, Anna Brózik, Ildikó Kasza, Katalin Német, Tamás I. Orbán, Csilla Özvegy-Laczka, András Váradi, Balázs Sarkadi

Research output: Contribution to journalArticle

14 Citations (Scopus)


The ATP-binding cassette (ABC) transporter ABCG2 plays an important role in tissue detoxification and confers multidrug resistance to cancer cells. Identification of expressional and functional cellular regulators of this multidrug transporter is therefore intensively pursued. The PI3-kinase/Akt signaling axis has been implicated as a key element in regulating various cellular functions, including the expression and plasma membrane localization of ABCG2. Here we demonstrate that besides inhibiting their respective target kinases, the pharmacological PI3-kinase inhibitor LY294002 and the downstream mTOR kinase inhibitor rapamycin also directly inhibit ABCG2 function. In contrast, wortmannin, another commonly used pharmacological inhibitor of PI3-kinase does not interact with the transporter. We suggest that direct functional modulation of ABCG2 should be taken into consideration when pharmacological agents are applied to dissect the specific role of PI3-kinase/Akt/mTOR signaling in cellular functions.

Original languageEnglish
Pages (from-to)869-874
Number of pages6
JournalBiochemical and biophysical research communications
Issue number4
Publication statusPublished - Apr 20 2012


  • ABCG2
  • LY294002
  • PI3-kinase/Akt/mTOR signaling
  • Rapamycin
  • Wortmannin

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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