Human ABCG2: Structure, function, and its role in multidrug resistance

Wei Mo, Jian Ting Zhang

Research output: Contribution to journalReview article

140 Scopus citations


Human ABCG2 is a member of the ATP-binding cassette (ABC) transporter superfamily and is known to contribute to multidrug resistance (MDR) in cancer chemotherapy. Among ABC transporters that are known to cause MDR, ABCG2 is particularly interesting for its potential role in protecting cancer stem cells and its complex oligomeric structure. Recent studies have also revealed that the biogenesis of ABCG2 could be modulated by small molecule compounds. These modulators, upon binding to ABCG2, accelerate the endocytosis and trafficking to lysosome for degradation and effectively reduce the half-life of ABCG2. Hence, targeting ABCG2 stability could be a new venue for therapeutic discovery to sensitize drug resistant human cancers. In this report, we review recent progress on understanding the structure, function, biogenesis, as well as physiological and pathophysiological functions of ABCG2.

Original languageEnglish (US)
Pages (from-to)1-27
Number of pages27
JournalInternational Journal of Biochemistry and Molecular Biology
Issue number1
StatePublished - Apr 18 2012


  • ATP-binding cassette
  • Cancer
  • Chemotherapy
  • Function
  • Human ABCG2
  • Multidrug resistance
  • Structure

ASJC Scopus subject areas

  • Molecular Biology
  • Biochemistry

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