Pharmacogenomics of the human ATP-binding cassette transporter ABCG2

Erin R. Gardner, William D. Figg, Alex Sparreboom*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

6 Scopus citations


Members of the ATP binding cassette transporter family are responsible for the cellular efflux of a broad range of endogenous compounds and xenobiotics in multiple tissues. The ABCG2 (ABCP, BCRP, MXR) protein, which is highly expressed in the gastrointestinal tract and liver as well as numerous multi-drug resistant cancer cells, is considered to be of particular importance in governing drug absorption, elimination and cellular sensitivity to a wide variety of clinically important drugs. A wealth of recent literature has also indicated that inhibition of this transporter may result in drug-drug interactions. Furthermore, genetic polymorphisms in the gene encoding ABCG2 have been described, which can significantly affect expression, cellular localization, and/or substrate recognition in vitro and in vivo. Alteration of ABCG2 transporter function by either of these mechanisms has been demonstrated to contribute to interindividual variability in drug disposition and treatment outcome (toxicity or response) with certain, but not all, substrates for ABCG2. In this report, we provide an update on this rapidly emerging field.

Original languageEnglish
Pages (from-to)331-344
Number of pages14
JournalCurrent Pharmacogenomics
Issue number4
StatePublished - Dec 2006
Externally publishedYes


  • ABCG2
  • Pharmacogenetics
  • Pharmacogenomics
  • Resistance
  • Transporter


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