ArticleCancer research2009
Identification of inhibitors of ABCG2 by a bioluminescence imaging-based high-throughput assay.
Article in Cancer research, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
22 citing papers in PubMed, 40 citations in OpenAlex.
- DeepICER: A deep learning framework for predicting compound-induced gene expression profiles.Acta pharmaceutica Sinica. B · 2026Article
- A Phenylfurocoumarin Derivative Reverses ABCG2-Mediated Multidrug Resistance In Vitro and In Vivo.International journal of molecular sciences · 2021Article
- HPVTranslational oncology · 2021Review
- Study on mechanism of elemene reversing tumor multidrug resistance based on luminescence pharmacokinetics in tumor cellsRSC advances · 2020Article
- Epithelial delamination is protective during pharmaceutical-induced enteropathy.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- In vitro characterization of pralidoxime transport and acetylcholinesterase reactivation across MDCK cells and stem cell-derived human brain microvascular endothelial cells (BC1-hBMECs).Fluids and barriers of the CNS · 2016Article
- The Drug Excipient Cyclodextrin Interacts With d-Luciferin and Interferes With Bioluminescence Imaging.Molecular imaging · 2016Article
- Molecular Imaging of Membrane Transporters' Activity in Cancer: a Picture is Worth a Thousand Tubes.The AAPS journal · 2015Review
- Identification of an old antibiotic clofoctol as a novel activator of unfolded protein response pathways and an inhibitor of prostate cancer.British journal of pharmacology · 2014Article
- Bioluminescent imaging of drug efflux at the blood-brain barrier mediated by the transporter ABCG2.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- Identification of cetrimonium bromide and irinotecan as compounds with synthetic lethality against NDRG1 deficient prostate cancer cells.Cancer biology & therapy · 2013Article
- Breast cancer resistance protein (BCRP/ABCG2): its role in multidrug resistance and regulation of its gene expression.Chinese journal of cancer · 2012Review
- Quantitative monitoring of mouse lung tumors by magnetic resonance imaging.Nature protocols · 2012Article
- Human ABCG2: structure, function, and its role in multidrug resistance.International journal of biochemistry and molecular biology · 2012Article
- Labeling of Luciferase/eGFP-expressing bone marrow-derived stromal cells with fluorescent micron-sized iron oxide particles improves quantitative and qualitative multimodal imaging of cellular grafts in vivo.Molecular imaging and biology · 2011Article
- ABCG2-dependent dye exclusion activity and clonal potential in epithelial cells continuously growing for 1 month from limbal explants.Investigative ophthalmology & visual science · 2011Article
- ATP-binding cassette transporters modulate both coelenterazine- and D-luciferin-based bioluminescence imaging.Molecular imaging · 2011Article
- The challenge of exploiting ABCG2 in the clinic.Current pharmaceutical biotechnology · 2011Review
- Continuing education course #1: non-invasive imaging as a problem-solving tool and translational biomarker strategy in toxicologic pathology.Toxicologic pathology · 2011Article
- Visualization and enrichment of live putative cancer stem cell populations following p53 inactivation or Bax deletion using non-toxic fluorescent dyes.Cancer biology & therapy · 2009Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
Abstract
ABCG2 is a member of the ATP-binding cassette (ABC) family of transporters, the overexpression of which is associated with tumor resistance to a variety of chemotherapeutic agents. Accordingly, combining ABCG2 inhibitor(s) with chemotherapy has the potential to improve treatment outcome. To search for clinically useful ABCG2 inhibitors, a bioluminescence imaging (BLI)-based assay was developed to allow high-throughput compound screening. This assay exploits our finding that d-luciferin, the substrate of firefly luciferase (fLuc), is a specific substrate of ABCG2, and ABCG2 inhibitors block the export of d-luciferin and enhance bioluminescence signal by increasing intracellular d-luciferin concentrations. HEK293 cells, engineered to express ABCG2 and fLuc, were used to screen the Hopkins Drug Library that includes drugs approved by the Food and Drug Administration (FDA) as well as drug candidates that have entered phase II clinical trials. Forty-seven compounds showed BLI enhancement, a measure of anti-ABCG2 activity, of > or =5-fold, the majority of which were not previously known as ABCG2 inhibitors. The assay was validated by its identification of known ABCG2 inhibitors and by confirming previously unknown ABCG2 inhibitors using established in vitro assays (e.g., mitoxantrone resensitization and BODIPY-prazosin assays). Glafenine, a potent new inhibitor, also inhibited ABCG2 activity in vivo. The BLI-based assay is an efficient method to identify new inhibitors of ABCG2. As they were derived from a FDA-approved compound library, many of the inhibitors uncovered in this study are ready for clinical testing.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.