ArticleBiochemical and biophysical research communications2009
Inhibition of human P-glycoprotein transport and substrate binding using a galantamine dimer.
Article in Biochemical and biophysical research communications, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 35 citations in OpenAlex.
- Galanthamine Fails to Reverse P-gp-Mediated Paclitaxel Resistance in Ovarian Cancer Cell Lines.Biomedicines · 2025Article
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- Fiscalin Derivatives as Potential Neuroprotective Agents.Pharmaceutics · 2022Article
- Potential Herb-Drug Interactions in the Management of Age-Related Cognitive Dysfunction.Pharmaceutics · 2021Review
- Studies on the Incompatibility betweenEvidence-based complementary and alternative medicine : eCAM · 2021Article
- The roles of the human ATP-binding cassette transporters P-glycoprotein and ABCG2 in multidrug resistance in cancer and at endogenous sites: future opportunities for structure-based drug design of inhibitors.Cancer drug resistance (Alhambra, Calif.) · 2021Article
- Genistein and Galantamine Combinations Decrease β-Amyloid PeptideNeurotoxicity research · 2020Article
- Phytochemicals: Potential Lead Molecules for MDR Reversal.Frontiers in pharmacology · 2020Review
- Ethnopharmacological Approaches for Dementia Therapy and Significance of Natural Products and Herbal Drugs.Frontiers in aging neuroscience · 2018Review
- Pathways and progress in improving drug delivery through the intestinal mucosa and blood-brain barriers.Therapeutic delivery · 2014Review
- Reversible dimers of the atypical antipsychotic quetiapine inhibit p-glycoprotein-mediated efflux in vitro with increased binding affinity and in situ at the blood-brain barrier.ACS chemical neuroscience · 2014Article
- Secondary Metabolites from Plants Inhibiting ABC Transporters and Reversing Resistance of Cancer Cells and Microbes to Cytotoxic and Antimicrobial Agents.Frontiers in microbiology · 2012Article
- A multivalent probe for AI-2 quorum-sensing receptors.Journal of the American Chemical Society · 2011Article
- Peptide-chlorambucil conjugates combat pgp-dependent drug efflux.ACS medicinal chemistry letters · 2011Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
The human multidrug resistance transporter P-glycoprotein (P-gp) prevents the entry of compounds into the brain by an active efflux mechanism at the blood-brain barrier (BBB). Treatment of neurodegenerative diseases, therefore, has become a challenge and the development of new reversible inhibitors of P-gp is pertinent to overcome this problem. We report the design and synthesis of a crosslinked agent based on the Alzheimer's disease treatment galantamine (Gal-2) that inhibits P-gp-mediated efflux from cultured cells. Gal-2 was found to inhibit the efflux of the fluorescent P-gp substrate rhodamine 123 in cancer cells that over-express P-gp with an IC(50) value of approximately 0.6 microM. In addition, Gal-2 was found to inhibit the efflux of therapeutic substrates of P-gp, such as doxorubicin, daunomycin and verapamil with IC(50) values ranging from 0.3 to 1.6 microM. Through competition experiments, it was determined that Gal-2 modulates P-gp mediated efflux by competing for the substrate binding sites. These findings support a potential role of agents, such as Gal-2, as inhibitors of P-gp at the BBB to augment treatment of neurodegenerative diseases.
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Registered trials
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