ArticleAnalytical biochemistry2013
Fluorescent substrates for flow cytometric evaluation of efflux inhibition in ABCB1, ABCC1, and ABCG2 transporters.
Article in Analytical biochemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 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.
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Who cites it
40 citing papers in PubMed, 65 citations in OpenAlex.
- Review
- Functional and Transcriptional Disruption of Hepatic ABC Transporters by Environmentally Relevant Short-Chain Per- and Polyfluoroalkyl Substances (PFAS).Journal of biochemical and molecular toxicology · 2025Article
- MDR1 promotes CD8 T cell persistence in tumors and protects against cytotoxic chemotherapy.bioRxiv : the preprint server for biology · 2025Article
- The proteostatic landscape of healthy human oocytes.The EMBO journal · 2025Article
- Ruxolitinib Modulates P-Glycoprotein Function, Delays T Cell Activation, and Impairs CCL19 Chemokine-Directed Migration in Human Cytotoxic T Lymphocytes.International journal of molecular sciences · 2025Article
- P-glycoprotein expression skews mitochondrial dye measurements in T cells.Frontiers in immunology · 2025Article
- Membrane-Fusing Vehicles for Re-Sensitizing Transporter-Mediated Multiple-Drug Resistance in Cancer.Pharmaceutics · 2024Article
- "Tumor Treating Fields" delivered via electromagnetic induction have varied effects across glioma cell lines and electric field amplitudes.American journal of cancer research · 2024Article
- Second-site suppressor mutations reveal connection between the drug-binding pocket and nucleotide-binding domain 1 of human P-glycoprotein (ABCB1).Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy · 2023Article
- Clinical and biological impact of ATP-binding cassette transporter activity in adult acute myeloid leukemia.Haematologica · 2023Article
- The Transporter-Mediated Cellular Uptake and Efflux of Pharmaceutical Drugs and Biotechnology Products: How and Why Phospholipid Bilayer Transport Is Negligible in Real Biomembranes.Molecules (Basel, Switzerland) · 2021Review
- A palette of fluorophores that are differentially accumulated by wild-type and mutant strains ofMicrobiology (Reading, England) · 2021Article
- Interactions of Potential Anti-COVID-19 Compounds with Multispecific ABC and OATP Drug Transporters.Pharmaceutics · 2021Article
- Disruption of small molecule transporter systems by Transporter-Interfering Chemicals (TICs).FEBS letters · 2020Review
- Review
- Structural Similarities between Some Common Fluorophores Used in Biology, Marketed Drugs, Endogenous Metabolites, and Natural Products.Marine drugs · 2020Article
- Inhibition of glycosphingolipid biosynthesis reverts multidrug resistance by differentially modulating ABC transporters in chronic myeloid leukemias.The Journal of biological chemistry · 2020Article
- Physiological expression and function of the MDR1 transporter in cytotoxic T lymphocytes.The Journal of experimental medicine · 2020Article
- Article
- A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.Molecular pharmacology · 2019Article
Corrections and comments
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Authors and funding
15 authors at 2 institutions in 1 country.
Funding
Abstract
ATP binding cassette (ABC) transmembrane efflux pumps such as P-glycoprotein (ABCB1), multidrug resistance protein 1 (ABCC1), and breast cancer resistance protein (ABCG2) play an important role in anticancer drug resistance. A large number of structurally and functionally diverse compounds act as substrates or modulators of these pumps. In vitro assessment of the affinity of drug candidates for multidrug resistance proteins is central to predict in vivo pharmacokinetics and drug-drug interactions. The objective of this study was to identify and characterize new substrates for these transporters. As part of a collaborative project with Life Technologies, 102 fluorescent probes were investigated in a flow cytometric screen of ABC transporters. The primary screen compared substrate efflux activity in parental cell lines with their corresponding highly expressing resistant counterparts. The fluorescent compound library included a range of excitation/emission profiles and required dual laser excitation as well as multiple fluorescence detection channels. A total of 31 substrates with active efflux in one or more pumps and practical fluorescence response ranges were identified and tested for interaction with eight known inhibitors. This screening approach provides an efficient tool for identification and characterization of new fluorescent substrates for ABCB1, ABCC1, and ABCG2.
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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.