ArticleScientific reports2018
Crown ethers reverse P-glycoprotein-mediated multidrug resistance in cancer cells.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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Who cites it
8 citing papers in PubMed, 31 citations in OpenAlex.
- Review
- Selective Inhibition of the ABCG2 Transporter by Primaquine Derivatives Reverses the Multidrug Resistance of Tumor Cells.International journal of molecular sciences · 2025Article
- Synthesis and Reactivity of Oligo(ethylene glycol)-Tethered Morita-Baylis-Hillman Dimers in the Formation of Macrocyclic Structures Showing Remarkable Cytotoxicity.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Differential Effect of Simulated Microgravity on the Cellular Uptake of Small Molecules.Pharmaceutics · 2024Article
- Cellular resistance mechanisms in cancer and the new approaches to overcome resistance mechanisms chemotherapy.Saudi medical journal · 2023Article
- Interaction of crown ethers with the ABCG2 transporter and their implication for multidrug resistance reversal.Histochemistry and cell biology · 2022Article
- Synthesis, Biological Evaluation, and Molecular Modeling of Aza-Crown Ethers.Molecules (Basel, Switzerland) · 2021Article
- Mechanisms of Multidrug Resistance in Cancer Chemotherapy.International journal of molecular sciences · 2020Review
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Multidrug resistance (MDR) is a widespread phenomenon exhibited by many cancers and represents a fundamental obstacle for successful cancer treatments. Tumour cells commonly achieve MDR phenotype through overexpression and/or increased activity of ABC transporters. P-glycoprotein transporter (P-gp, ABCB1) is a major cause of MDR and therefore represents a valuable target for MDR reversal. Several naturally occurring potassium ionophores (e.g. salinomycin) were shown to inhibit P-gp effectively. We have previously shown antitumour activity of a number of 18-crown-6 ether compounds that transport potassium ions across membranes. Here we present data on P-gp inhibitory activity of 16 adamantane-substituted monoaza- and diaza-18-crown-6 ether compounds, and their effect on MDR reversal in model cell lines. We show that crown ether activity depends on their lipophilicity as well as on the linker to adamantane moiety. The most active crown ethers were shown to be more effective in sensitising MDR cells to paclitaxel and adriamycin than verapamil, a well-known P-gp inhibitor. Altogether our data demonstrate a novel use of crown ethers for inhibition of P-gp and reversal of MDR phenotype.
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Registered trials
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