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Related Experiment Video

Updated: Jul 11, 2026

Dual Bioluminescence Imaging of Tumor Progression and Angiogenesis
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ABCG2/BCRP expression modulates D-Luciferin based bioluminescence imaging.

Yimao Zhang1, Joseph P Bressler, Jeff Neal

  • 1Russell H. Morgan Department of Radiology, The Johns Hopkins Bloomberg School of Public Health, The Johns Hopkins School of Medicine, Baltimore, Maryland, USA.

Cancer Research
|October 3, 2007
PubMed
Summary

The ATP-binding cassette transporter ABCG2/BCRP affects bioluminescence imaging (BLI) signal output using d-luciferin. This finding is crucial for accurate in vivo BLI and may reveal new ABCG2/BCRP inhibitor discovery methods.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Medical Imaging

Background:

  • Bioluminescence imaging (BLI) is vital for studying transgene expression and in vivo disease models.
  • The d-luciferin/firefly luciferase (fLuc) system is preferred for in vivo BLI due to photon emission properties.
  • ATP-binding cassette (ABC) transporters influence cellular drug and substrate transport.

Purpose of the Study:

  • To investigate the impact of ABCG2/BCRP expression on d-luciferin-based BLI signal output.
  • To determine if d-luciferin is a substrate for ABCG2/BCRP and other ABC transporters.
  • To explore the implications of ABCG2/BCRP activity for in vivo BLI accuracy and drug discovery.

Main Methods:

  • In vitro enzyme assays to test d-luciferin as a substrate for ABCG2/BCRP and other transporters (ABCB1/Pgp, ABCC1/MRP1, ABCC2/MRP2).

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  • Cellular uptake studies of d-luciferin, modulated by ABC transporter inhibitors like fumitremorgin C.
  • In vivo BLI of xenografts engineered to express ABCG2/BCRP or derived from naturally expressing cancer cell lines.

    • Main Results:

    • d-Luciferin was identified as a substrate for ABCG2/BCRP, but not for ABCB1/Pgp, ABCC1/MRP1, or ABCC2/MRP2.
    • Inhibitors of ABCG2/BCRP modulated d-luciferin uptake in cells.
    • Expression and function of ABCG2/BCRP in xenografts significantly affected d-luciferin-dependent BLI signals in vivo.

    Conclusions:

    • ABCG2/BCRP actively transports d-luciferin, impacting BLI signal intensity.
    • Consideration of ABCG2/BCRP activity is essential for accurate interpretation of d-luciferin-based BLI data.
    • This research suggests novel strategies for high-throughput screening of ABCG2/BCRP inhibitors.