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Suppression of ABCG2 inhibits cancer cell proliferation

Zhong Chen1, Fang Liu, Qian Ren

  • 1State Key Laboratory of Experimental Hematology, Institute of Hematology & Hospital of Blood Diseases, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin, People's Republic of China.

International Journal of Cancer
|July 31, 2009
PubMed

Insights

The ATP-binding cassette efflux transporter, ABCG2, regulates cancer cell proliferation. Inhibiting ABCG2 function halts cancer cell growth by affecting the cell cycle, revealing a new role for this transporter.

Area of Science:

  • Molecular Biology
  • Cancer Research
  • Cell Biology

Background:

  • ABCG2 (ATP-binding cassette subfamily G member 2) is an efflux transporter found in various tissues, stem cells, and cancer cells.
  • ABCG2 is known to maintain stem cell phenotype and contribute to multidrug resistance in cancer.
  • Its role in other cellular processes, particularly cancer cell proliferation, is not well understood.

Purpose of the Study:

  • To investigate the role of ABCG2 in cancer cell proliferation.
  • To elucidate the mechanisms by which ABCG2 influences cell cycle progression in cancer cells.

Main Methods:

  • RNA interference (RNAi) was used to down-regulate ABCG2 expression in MCF-7/MX and A549 cancer cell lines.
  • Cell proliferation was assessed following ABCG2 knockdown.
  • Cell cycle analysis was performed using flow cytometry.
  • Expression levels of cell cycle regulatory proteins (cyclin D3, p21) were analyzed.
  • Chemical inhibition of ABCG2 function using fumitremorgin C was employed to study its effects on proliferation.

Main Results:

  • Down-regulation of ABCG2 significantly inhibited the proliferation of MCF-7/MX and A549 cells.
  • ABCG2 knockdown led to a decrease in cells within the S phase and an accumulation of cells in the G0/G1 phase.
  • The observed G0/G1 growth arrest was linked to reduced cyclin D3 and increased p21 expression.
  • Pharmacological inhibition of ABCG2 also resulted in decreased cell proliferation and prolonged G0/G1 phase.

Conclusions:

  • ABCG2 plays a significant role in regulating cancer cell proliferation.
  • ABCG2 influences cell cycle progression, specifically promoting entry into and progression through the S phase.
  • These findings identify a novel function of ABCG2 in the context of cancer cell proliferation, beyond its known roles in stemness and drug resistance.

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