Robert W. Robey, Sabrina Lusvarghi, Cindy H. Chau, Agnes Basseville, William D. Figg, Suresh V. Ambudkar, Susan E. Bates

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review


The ABCG2 half-transporter plays an important in normal physiology predominantly in protective roles at the maternal-fetal barrier and the blood-brain barrier and affects oral bioavailability of substrates. High expression in some cancers suggests it may also play a role in multidrug resistance in cancer. Polymorphic variants have been shown to impair trafficking of the protein to the cell surface, with the Q141K variant being associated with a higher incidence of gout. Loss of ABCG2 expression forms the genetic bases of the Jr(a-) blood type. This chapter will focus on more recent ABCG2 studies with particular focus on genetic variants and atomic structures. These more recent findings may lead to a better understanding of the function of ABCG2, potentially leading to the development of better inhibitors or to the development of compounds that are not substrates for the transporter.

Original languageEnglish
Title of host publicationDrug Transporters
Subtitle of host publicationMolecular Characterization and Role in Drug Disposition: Third Edition
Number of pages22
ISBN (Electronic)9781119739883
ISBN (Print)9781119737551
StatePublished - 1 Jan 2022
Externally publishedYes


  • ABCG2
  • ATP-binding cassette transporter
  • BCRP
  • blood-brain barrier
  • drug disposition
  • drug resistance
  • gout
  • oral bioavailability
  • placenta
  • polymorphism
  • stem cells
  • urate


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