Human ABCG2

Structure, function, and its role in multidrug resistance

Wei Mo, Jian-Ting Zhang

Research output: Contribution to journalArticle

112 Citations (Scopus)

Abstract

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
Pages (from-to)1-27
Number of pages27
JournalInternational Journal of Biochemistry and Molecular Biology
Volume3
Issue number1
StatePublished - 2012

Fingerprint

ATP-Binding Cassette Transporters
Multiple Drug Resistance
Chemotherapy
Neoplastic Stem Cells
Endocytosis
Lysosomes
Stem cells
Modulators
Half-Life
Neoplasms
Drug Therapy
Degradation
Molecules
Pharmaceutical Preparations
Therapeutics

Keywords

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

ASJC Scopus subject areas

  • Molecular Biology
  • Biochemistry

Cite this

Human ABCG2 : Structure, function, and its role in multidrug resistance. / Mo, Wei; Zhang, Jian-Ting.

In: International Journal of Biochemistry and Molecular Biology, Vol. 3, No. 1, 2012, p. 1-27.

Research output: Contribution to journalArticle

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