ArticleBiochemical pharmacology2016
Cooperativity between verapamil and ATP bound to the efflux transporter P-glycoprotein.
Article in Biochemical pharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.
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Who cites it
37 citing papers in PubMed.
- Metabolic crisis and TRPM4 activation cause QT prolongation in TANGO2 deficiency disorder.Cardiovascular research · 2026Article
- Self-assembled verteporfin nanoparticles decrease drug efflux by P-glycoprotein without light activation in drug-resistant cancer cells.Bioengineering & translational medicine · 2026Article
- Assessment of Intramuscular Verapamil as Pharmacological Countermeasure in a Rat Model of Organophosphate DFP-induced Status Epilepticus.Neurotoxicity research · 2025Article
- Elucidating the Complex Structural and Molecular Mechanisms Driving P-Glycoprotein-Mediated Transport of Cardiac Glycosides.International journal of molecular sciences · 2025Article
- Selective Inhibition of the ABCG2 Transporter by Primaquine Derivatives Reverses the Multidrug Resistance of Tumor Cells.International journal of molecular sciences · 2025Article
- Verapamil and its metabolite norverapamil inhibit theProceedings of the National Academy of Sciences of the United States of America · 2025Article
- Cryo-EM of human P-glycoprotein reveals an intermediate occluded conformation during active drug transport.Nature communications · 2025Article
- Progress in Research of Nanotherapeutics for Overcoming Multidrug Resistance in Cancer.International journal of molecular sciences · 2024Review
- Human gut Actinobacteria boost drug absorption by secreting P-glycoprotein ATPase inhibitors.iScience · 2024Article
- Utilizing surface plasmon resonance as a novel method for monitoringFrontiers in biophysics · 2024Article
- Genetics ofCancers · 2023Review
- Advantages and potential limitations of applying AFM kymograph analysis to pharmaceutically relevant membrane proteins in lipid bilayers.Scientific reports · 2023Article
- Coleon U, Isolated fromPharmaceutics · 2023Article
- The human proton pump inhibitors inhibitProceedings of the National Academy of Sciences of the United States of America · 2023Article
- Interaction of a Homologous Series of Amphiphiles with P-glycoprotein in a Membrane Environment-Contributions of Polar and Non-Polar Interactions.Pharmaceutics · 2023Article
- Four Decades of Cytochrome P450 2B Research: From Protein Adducts to Protein Structures and Beyond.Drug metabolism and disposition: the biological fate of chemicals · 2023Review
- The History of the ABC Proteins in Human Trypanosomiasis Pathogens.Pathogens (Basel, Switzerland) · 2022Review
- Targeting the two-pore channel 2 in cancer progression and metastasis.Exploration of targeted anti-tumor therapy · 2022Review
- Novel Sigma-2 receptor ligand A011 overcomes MDR in adriamycin-resistant human breast cancer cells by modulating ABCB1 and ABCG2 transporter function.Frontiers in pharmacology · 2022Article
- Acquired Drug Resistance Enhances Imidazoquinoline Efflux by P-Glycoprotein.Pharmaceuticals (Basel, Switzerland) · 2021Article
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4 authors.
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Abstract
The P-glycoprotein (Pgp) transporter plays a central role in drug disposition by effluxing a chemically diverse range of drugs from cells through conformational changes and ATP hydrolysis. A number of drugs are known to activate ATP hydrolysis of Pgp, but coupling between ATP and drug binding is not well understood. The cardiovascular drug verapamil is one of the most widely studied Pgp substrates and therefore, represents an ideal drug to investigate the drug-induced ATPase activation of Pgp. As previously noted, verapamil-induced Pgp-mediated ATP hydrolysis kinetics was biphasic at saturating ATP concentrations. However, at subsaturating ATP concentrations, verapamil-induced ATPase activation kinetics became monophasic. To further understand this switch in kinetic behavior, the Pgp-coupled ATPase activity kinetics was checked with a panel of verapamil and ATP concentrations and fit with the substrate inhibition equation and the kinetic fitting software COPASI. The fits suggested that cooperativity between ATP and verapamil switched between low and high verapamil concentration. Fluorescence spectroscopy of Pgp revealed that cooperativity between verapamil and a non-hydrolyzable ATP analog leads to distinct global conformational changes of Pgp. NMR of Pgp reconstituted in liposomes showed that cooperativity between verapamil and the non-hydrolyzable ATP analog modulate each other's interactions. This information was used to produce a conformationally-gated model of drug-induced activation of Pgp-mediated ATP hydrolysis.
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