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

Junkang Xu1, Hui Peng, Jian-Ting Zhang

  • 1Department of Pharmacology and Toxicology, Indiana University Cancer Center, Walther Oncology Center/Walther Cancer Institute, Indiana University School of Medicine, Indianapolis, IN 46202, USA.

Current Medicinal Chemistry
|March 10, 2007
PubMed

Insights

The human ABCG2 transporter is crucial for drug absorption and elimination, and its role in multidrug resistance in cancer chemotherapy is significant. Inhibiting ABCG2 shows promise for enhancing chemotherapy effectiveness.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Human ABCG2, an ATP-binding cassette transporter, is widely distributed in key organs like the placenta, liver, and brain.
  • Its strategic localization suggests a vital role in the absorption, distribution, and elimination of xenobiotics and drugs.
  • Elevated ABCG2 expression in various cancers points to its involvement in multidrug resistance (MDR).

Purpose of the Study:

  • To review current knowledge on human ABCG2.
  • To explore its relevance in drug disposition and multidrug resistance.
  • To summarize known ABCG2 substrates and inhibitors.

Main Methods:

  • Literature review of studies on ABCG2 function, expression, and substrate/inhibitor profiles.
  • Analysis of the role of ABCG2 in physiological transport and cancer drug resistance.

Main Results:

  • ABCG2 actively transports a diverse range of organic molecules and anticancer drugs.
  • Inhibition or modulation of ABCG2 function/expression can potentially overcome drug resistance.
  • Numerous ABCG2 substrates and inhibitors have been identified.

Conclusions:

  • Human ABCG2 is a critical transporter with significant implications for drug disposition and cancer chemotherapy.
  • Targeting ABCG2 presents a viable strategy for developing novel therapeutic approaches to combat multidrug resistance.
  • Further research into ABCG2 substrates and inhibitors is essential for clinical applications.

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