Screening Compounds with a Novel High-Throughput ABCB1-Mediated Efflux Assay Identifies Drugs with Known Therapeutic Targets at Risk for Multidrug Resistance Interference
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ABCB1, also known as P-glycoprotein (P-gp) or multidrug resistance protein 1 (MDR1), is a membrane-associated multidrug transporter of the ATP-binding cassette (ABC) transporter family. It is one of the most widely studied transporters that enable cancer cells to develop drug resistance. Reliable high-throughput assays that can identify compounds that interact with ABCB1 are crucial for developing new therapeutic drugs. A high-throughput assay for measuring ABCB1-mediated calcein AM efflux was developed using a fluorescent and phase-contrast live cell imaging system. This assay demonstrated the time- and dose-dependent accumulation of fluorescent calcein in ABCB1-overexpressing KB-V1 cells. Validation of the assay was performed with known ABCB1 inhibitors, XR9576, verapamil, and cyclosporin A, all of which displayed dose-dependent inhibition of ABCB1-mediated calcein AM efflux in this assay. Phase-contrast and fluorescent images taken by the imaging system provided additional opportunities for evaluating compounds that are cytotoxic or produce false positive signals. Compounds with known therapeutic targets and a kinase inhibitor library were screened. The assay identified multiple agents as inhibitors of ABCB1-mediated efflux and is highly reproducible. Among compounds identified as ABCB1 inhibitors, BEZ235, BI 2536, IKK 16, and ispinesib were further evaluated. The four compounds inhibited calcein AM efflux in a dose-dependent manner and were also active in the flow cytometry-based calcein AM efflux assay. BEZ235, BI 2536, and IKK 16 also successfully inhibited the labeling of ABCB1 with radiolabeled photoaffinity substrate [(125)I]iodoarylazidoprazosin. Inhibition of ABCB1 with XR9576 and cyclosporin A enhanced the cytotoxicity of BI 2536 to ABCB1-overexpressing cancer cells, HCT-15-Pgp, and decreased the IC50 value of BI 2536 by several orders of magnitude. This efficient, reliable, and simple high-throughput assay has identified ABCB1 substrates/inhibitors that may influence drug potency or drug-drug interactions and predict multidrug resistance in clinical treatment.
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Several kinase inhibitors have been shown to be potent inhibitors of MDR1 drug efflux activity capable of overcoming multidrug resistance in cancer cells.
“Notably, several kinase inhibitors have been shown to be potent inhibitors of MDR1 drug efflux activity capable of overcoming multidrug resistance in cancer cells (35).”
From The drug efflux pump MDR1 promotes intrinsic and acquired resistance to PROTACs in cancer cells (2022) · cites this paper as [35]
Several kinase inhibitors, including FDA-approved kinase inhibitors, have been shown to directly inhibit MDR1 drug efflux activity.
“Several kinase inhibitors have been shown to directly inhibit MDR1 drug efflux activity, including a number of FDA-approved kinase inhibitors (35, 52).”
From The drug efflux pump MDR1 promotes intrinsic and acquired resistance to PROTACs in cancer cells (2022) · cites this paper as [35]
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The Discovery and Development of Eg5 Inhibitors for the Clinic
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Targeting Cancer Stem Cells: New Perspectives for a Cure to Cancer
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Orphan drugs for myelofibrosis
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Isoreserpine Reverses Multidrug Resistance Mediated by ABCB1
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Analysis of transporter activity in an Alzheimer’s disease blood-brain barrier cell model
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ABCB1 overexpression confers resistance to litronesib, an Eg5 inhibitor
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- Authors
- Ansbro, M. R., Shukla, S., Ambudkar, S. V., Yuspa, S. H., & Li, L.
- Affiliations
- National Cancer Institute (US)
- Corresponding author
- Li, Luowei
- Venue
- PLoS ONE
- Publisher
- Public Library of Science (PLoS)
- Published
- 2013-04-10
- Volume
- 8
- Issue
- 4
- Pages
- e60334
- ISSN
- 1932-6203 (ISSN-L)
- PMC
- PMC3622673
- OpenAlex
- W1984802696
- Cited by
- 54
- References
- 50
- Citations by year
- 2026: 2 · 2025: 3 · 2024: 6 · 2023: 3 · 2022: 4 · 2021: 1 · 2020: 5 · 2019: 2 · 2018: 3 · 2017: 4 · 2016: 3 · 2015: 9 · 2014: 6 · 2013: 3
- FWCI
- 3.75
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- PLoS ONE (publishedVersion, public-domain)
- Europe PMC (PubMed Central) (publishedVersion, other-oa)
- PubMed Central (publishedVersion, public-domain)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Figshare (submittedVersion, cc-by)
- Funders
- National Institutes of Health
- National Cancer Institute
- Topics
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Medicine › Antibiotic Resistance in Bacteria
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Keywords
- P-glycoprotein, multidrug resistance, high-throughput assay, ABC transporter inhibitors, drug-drug interactions, BEZ235, BI2536, ispinesib, photoaffinity labeling, drug resistance prediction
- MeSH terms
- Cell Line, Humans, Quinolines, Verapamil, Reproducibility of Results, Cyclosporine, Drug Resistance, Multiple, ATP Binding Cassette Transporter, Subfamily B, ATP Binding Cassette Transporter, Subfamily B, Member 1, High-Throughput Screening Assays
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Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
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