Evidence map›Paper›PMID 24297888›Full record

ArticleProceedings of the National Academy of Sciences of the United States of America2013

Bioluminescent imaging of drug efflux at the blood-brain barrier mediated by the transporter ABCG2.

Joshua Bakhsheshian, Bih-Rong Wei, Ki-Eun Chang, Suneet Shukla, Suresh V Ambudkar, R Mark Simpson, Michael M Gottesman, Matthew D Hall

Open access · bronzeAbstract read
In one paragraph

Article in Proceedings of the National Academy of Sciences of the United States of America, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.

0numbers the graph read from it
0cells of the map it votes in
32citing papers in PubMed
2.7field-weighted citation impact, top 9% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

32 citing papers in PubMed, 45 citations in OpenAlex.

  1. Trial
  2. Article
  3. Article
  4. Review
  5. Progress in characterizing ABC multidrug transporters in zebrafish.Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy · 2024
    Article
  6. Article
  7. Article
  8. Article
  9. Article
  10. Article
  11. New mechanisms of multidrug resistance: an introduction to theCancer drug resistance (Alhambra, Calif.) · 2023
    Article
  12. Review
  13. Factors Influencing Luciferase-Based Bioluminescent Imaging in Preclinical Models of Brain Tumor.Drug metabolism and disposition: the biological fate of chemicals · 2022
    Article
  14. Article
  15. Article
  16. Review
  17. Review
  18. Influence of breast cancer resistance protein and P-glycoprotein on tissue distribution and excretion of Ko143 assessed with PET imaging in mice.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2018
    Article
  19. Review
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors at 3 institutions in 1 country.

Joshua BakhsheshianLaboratory of Cell Biology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892.
Bih-Rong Wei
Ki-Eun Chang
Suneet Shukla
Suresh V Ambudkar
R Mark Simpson
Michael M Gottesman
Matthew D Hall
National Cancer Institute · USCenter for Cancer Research · USNational Institutes of Health · US

Funding

Molecular Pathology Research for Cancer Diagnostics and BiomarkersZICBC010953 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI SIMPSON, ROBERT · 2009 to 2025
$22.9M
Howard Hughes Medical InstituteIntramural NIH HHS
6 · The paper itself

Abstract

ATP-binding cassette (ABC) transporters are a group of transmembrane proteins that maintain chemical homeostasis through efflux of compounds out of organelles and cells. Among other functions, ABC transporters play a key role in protecting the brain parenchyma by efflux of xenobiotics from capillary endothelial cells at the blood-brain barrier (BBB). They also prevent the entry of therapeutic drugs at the BBB, thereby limiting their efficacy. One of the key transporters playing this role is ABCG2. Although other ABC transporters can be studied through various imaging modalities, no specific probe exists for imaging ABCG2 function in vivo. Here we show that D-luciferin, the endogenous substrate of firefly luciferase, is a specific substrate for ABCG2. We hypothesized that ABCG2 function at the BBB could be evaluated by using bioluminescence imaging in transgenic mice expressing firefly luciferase in the brain. Bioluminescence signal in the brain of mice increased with coadministration of the ABCG2 inhibitors Ko143, gefitinib, and nilotinib, but not an ABCB1 inhibitor. This method for imaging ABCG2 function at the BBB will facilitate understanding of the function and pharmacokinetic inhibition of this transporter.

Indexed as

Luminescent Measurements3T3 CellsAdenosineAnimalsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily B, Member 1ATP Binding Cassette Transporter, Subfamily G, Member 2Blood-Brain BarrierCell Line, TumorDiketopiperazinesEndothelial CellsFirefly LuciferinGefitinibGene ExpressionHEK293 Cells3-(6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino(1',2'-1,6)pyrido(3,4-b)indol-3-yl)propionic acid tert-butyl esterABCB1 protein, humanABCG2 protein, humanAbcg2 protein, mouseAdenosineATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily B, Member 1ATP Binding Cassette Transporter, Subfamily G, Member 2DiketopiperazinesFirefly LuciferinGefitinibHeterocyclic Compounds, 4 or More RingsLuciferases, FireflyLuminescent AgentsNeoplasm ProteinsnilotinibProtein Kinase InhibitorsPyrimidinesQuinazolinesXenobiotics

Identifiers

PMID24297888
PMCPMC3870704
OpenAlexW2057143539

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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.