Evidence map›Paper›PMID 31371421›Full record

ArticleDrug metabolism and disposition: the biological fate of chemicals2019

Synthesis and Characterization of Bodipy-FL-Cyclosporine A as a Substrate for Multidrug Resistance-Linked P-Glycoprotein (ABCB1).

Andaleeb Sajid, Natarajan Raju, Sabrina Lusvarghi, Shahrooz Vahedi, Rolf E Swenson, Suresh V Ambudkar

Open access · bronzeAbstract read
In one paragraph

Article in Drug metabolism and disposition: the biological fate of chemicals, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
1.1field-weighted citation impact, top 20% 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

12 citing papers in PubMed, 18 citations in OpenAlex.

  1. Article
  2. Manipulating anthracyclines for deeper tissue penetration and implications for glycolytic tissues.Proceedings of the National Academy of Sciences of the United States of America · 2025
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  10. Reversing the direction of drug transport mediated by the human multidrug transporter P-glycoprotein.Proceedings of the National Academy of Sciences of the United States of America · 2020
    Article
  11. Article
  12. Review
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

6 authors at 3 institutions in 1 country.

Andaleeb SajidLaboratory of Cell Biology, Center for Cancer Research, National Cancer Institute (A.S., S.L., S.V., S.V.A.), and Imaging Probe Development Center, National Heart, Lung and Blood Institute (N.R., R.E.S.), National Institutes of Health, Bethesda, Maryland.
Natarajan RajuLaboratory of Cell Biology, Center for Cancer Research, National Cancer Institute (A.S., S.L., S.V., S.V.A.), and Imaging Probe Development Center, National Heart, Lung and Blood Institute (N.R., R.E.S.), National Institutes of Health, Bethesda, Maryland.
Sabrina LusvarghiLaboratory of Cell Biology, Center for Cancer Research, National Cancer Institute (A.S., S.L., S.V., S.V.A.), and Imaging Probe Development Center, National Heart, Lung and Blood Institute (N.R., R.E.S.), National Institutes of Health, Bethesda, Maryland.
Shahrooz VahediLaboratory of Cell Biology, Center for Cancer Research, National Cancer Institute (A.S., S.L., S.V., S.V.A.), and Imaging Probe Development Center, National Heart, Lung and Blood Institute (N.R., R.E.S.), National Institutes of Health, Bethesda, Maryland.
Rolf E SwensonLaboratory of Cell Biology, Center for Cancer Research, National Cancer Institute (A.S., S.L., S.V., S.V.A.), and Imaging Probe Development Center, National Heart, Lung and Blood Institute (N.R., R.E.S.), National Institutes of Health, Bethesda, Maryland.
Suresh V AmbudkarLaboratory of Cell Biology, Center for Cancer Research, National Cancer Institute (A.S., S.L., S.V., S.V.A.), and Imaging Probe Development Center, National Heart, Lung and Blood Institute (N.R., R.E.S.), National Institutes of Health, Bethesda, Maryland ambudkar@mail.nih.gov.
National Heart Lung and Blood Institute · USNational Cancer Institute · USNational Institutes of Health · US

Funding

Imaging Probe Development CenterZICHL005090 · NHLBI · NATIONAL HEART, LUNG, AND BLOOD INSTITUTE · PI SWENSON, ROLF · 2011 to 2025
$22.2M
6 · The paper itself

Abstract

Fluorescent conjugates of drugs can be used to study cellular functions and pharmacology. These compounds interact with proteins as substrates or inhibitors, helping in the development of unique fluorescence-based methods to study in vivo localization and molecular mechanisms. P-glycoprotein (P-gp, ABCB1) is an ATP-binding cassette (ABC) transporter that effluxes most anticancer drugs from cells, contributing to the development of drug resistance. To study the transport function of P-gp, we synthesized a Bodipy-labeled fluorescent conjugate of cyclosporine A (BD-CsA). After synthesis and characterization of its chemical purity, BD-CsA was compared with the commonly used 7-nitrobenz-2-oxa-1,3-diazol-4-yl (NBD)-CsA probe. In flow cytometry assays, the fluorescence intensity of BD-CsA was almost 10 times greater than that of NBD-CsA, enabling us to use significantly lower concentrations of BD-CsA to achieve the same fluorescence levels. We found that BD-CsA is recognized as a transport substrate by both human and mouse P-gp. The rate of efflux of BD-CsA by human P-gp is comparable to that of NBD-CsA. The transport of BD-CsA was inhibited by tariquidar, with similar IC

Indexed as

Antineoplastic AgentsATP Binding Cassette Transporter, Subfamily BAzolesBoron CompoundsCyclosporineDrug Resistance, MultipleDrug Resistance, NeoplasmFlow CytometryFluorescent DyesHeLa CellsHumansInhibitory Concentration 50Microscopy, FluorescenceMolecular Docking SimulationMolecular ImagingMolecular Probes4,4-difluoro-4-bora-3a,4a-diaza-s-indacene7-nitrobenz-2-oxa-1,3-diazol-4-ylABCB1 protein, humanAntineoplastic AgentsATP Binding Cassette Transporter, Subfamily BAzolesBoron CompoundsCyclosporineFluorescent DyesMolecular ProbesNitrobenzenesQuinolinesRecombinant Proteinstariquidar

Identifiers

PMID31371421
PMCPMC6744393
OpenAlexW2965444452

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.