Human multidrug transporter ABCG2, a target for sensitizing drug resistance in cancer chemotherapy

Junkang Xu, Hui Peng, Jian-Ting Zhang

Research output: Contribution to journalArticle

33 Citations (Scopus)

Abstract

Human ABCG2, a member of the ATP-binding cassette transporter superfamily which transports a wide variety of substrates, is highly expressed in placental syncytiotrophoblasts, in the canalicular membranes of liver, in the apical membrane of the small intestine epithelium, and at the luminal surface of the endothelial cells of human brain micro vessels. This strategic tissue localization indicates that ABCG2 plays an important role in absorption, distribution, and elimination of xenobiotics and drugs. High ABCG2 expression has also been detected in many hematological malignancies and solid tumors, indicating that ABCG2 is likely responsible also for the multidrug resistance in cancer chemotherapy. Indeed, ABCG2 can actively transport structurally diverse conjugated- or unconjugated-organic molecules and various anticancer drugs. Many chemo-sensitizing agents have been discovered, which can be developed for increasing drug adsorption and reversing drug resistance in cancer chemotherapy by inhibiting ABCG2 function or expression. This review summarizes current knowledge on ABCG2, its relevance to multidrug resistance and drug disposition, and its evergrowing numbers of substrates and inhibitors.

Original languageEnglish
Pages (from-to)689-701
Number of pages13
JournalCurrent Medicinal Chemistry
Volume14
Issue number6
DOIs
StatePublished - Mar 2007

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Chemotherapy
Drug Resistance
Drug Therapy
Multiple Drug Resistance
Pharmaceutical Preparations
Neoplasms
ATP-Binding Cassette Transporters
Membranes
Trophoblasts
Xenobiotics
Hematologic Neoplasms
Adsorption
Small Intestine
Endothelial cells
Substrates
Epithelium
Endothelial Cells
Liver
Tumors
Brain

Keywords

  • ABC transporter
  • ABCG2
  • Chemo-sensitization
  • Drug resistance
  • Inhibitors
  • MDR
  • Oligomerization
  • Substrates

ASJC Scopus subject areas

  • Organic Chemistry
  • Biochemistry, Genetics and Molecular Biology(all)
  • Biochemistry
  • Pharmacology

Cite this

Human multidrug transporter ABCG2, a target for sensitizing drug resistance in cancer chemotherapy. / Xu, Junkang; Peng, Hui; Zhang, Jian-Ting.

In: Current Medicinal Chemistry, Vol. 14, No. 6, 03.2007, p. 689-701.

Research output: Contribution to journalArticle

Xu, Junkang ; Peng, Hui ; Zhang, Jian-Ting. / Human multidrug transporter ABCG2, a target for sensitizing drug resistance in cancer chemotherapy. In: Current Medicinal Chemistry. 2007 ; Vol. 14, No. 6. pp. 689-701.
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