Cooperativity between verapamil and ATP bound to the efflux transporter P-glycoprotein.

No abstract is available for this paper.

• Publication year

  2016

• Venue

  Biochemical Pharmacology

• Publication date

  2016-10-15

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/j.bcp.2016.08.013PMID 27531061PMCID PMC5341695
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Unravelling the complex drug–drug interactions of the cardiovascular drugs, verapamil and digoxin, with P-glycoprotein

  2016influential reference
• Enzyme Kinetics And Mechanism

  2016cited by this paper
• Cryo-EM Analysis of the Conformational Landscape of Human P-glycoprotein (ABCB1) During its Catalytic Cycle

  2016cited by this paper
• Structural basis for allosteric cross-talk between the asymmetric nucleotide binding sites of a heterodimeric ABC exporter

  2014cited by this paper
• Pharmacokinetic variability of flecainide in younger Japanese patients and mechanisms for renal excretion and intestinal absorption

  2014cited by this paper
• The P-glycoprotein transport system and cardiovascular drugs.

  2013cited by this paper
• Crystal structure of the multidrug transporter P-glycoprotein from Caenorhabditis elegans

  2012cited by this paper
• Use of NMR saturation transfer difference spectroscopy to study ligand binding to membrane proteins.

  2012cited by this paper
• Crystal structure of the multidrug transporter P-glycoprotein from C. elegans

  2012cited by this paper
• The ATPase Activity of the P-glycoprotein Drug Pump Is Highly Activated When the N-terminal and Central Regions of the Nucleotide-binding Domains Are Linked Closely Together*

  2012cited by this paper
• Intracellular ATP levels are a pivotal determinant of chemoresistance in colon cancer cells.

  2012cited by this paper
• Conformational Analysis of Human ATP-binding Cassette Transporter ABCB1 in Lipid Nanodiscs and Inhibition by the Antibodies MRK16 and UIC2*

  2011cited by this paper
• A Gene Optimization Strategy that Enhances Production of Fully Functional P-Glycoprotein in Pichia pastoris

  2011cited by this paper
• Dynamic Ligand-induced Conformational Rearrangements in P-glycoprotein as Probed by Fluorescence Resonance Energy Transfer Spectroscopy*

  2011cited by this paper
• The structural basis for homotropic and heterotropic cooperativity of midazolam metabolism by human cytochrome P450 3A4.

  2011cited by this paper
• Physiological levels of ATP negatively regulate proteasome function

  2010cited by this paper
• Characterization of an Asymmetric Occluded State of P-glycoprotein with Two Bound Nucleotides

  2010cited by this paper
• ABC Transporters and Multidrug Resistance

  2009cited by this paper
• CHARACTERIZATION OF AN ASYMMETRIC OCCLUDED STATE OF P-GLYCOPROTEIN WITH TWO BOUND NUCLEOTIDES: IMPLICATIONS FOR CATALYSIS*

  2009cited by this paper
• Structure of P-Glycoprotein Reveals a Molecular Basis for Poly-Specific Drug Binding

  2009cited by this paper
• Molecular models of human P-glycoprotein in two different catalytic states

  2009cited by this paper
• Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition

  2008cited by this paper
• Validation and application of Caco-2 assays for the in vitro evaluation of development candidate drugs as substrates or inhibitors of P-glycoprotein to support regulatory submissions

  2008cited by this paper
• Structure-based interpretation of the mutagenesis database for the nucleotide binding domains of P-glycoprotein.

  2008cited by this paper
• Uptake or extrusion: crystal structures of full ABC transporters suggest a common mechanism

  2007influential reference
• BioMagResBank

  2007cited by this paper
• P-Glycoprotein kinetics measured in plasma membrane vesicles and living cells.

  2007cited by this paper
• Flexibility in the ABC transporter MsbA: Alternating access with a twist

  2007influential reference
• Direct detection of ligand binding to Sepharose-immobilised protein using saturation transfer double difference (STDD) NMR spectroscopy.

  2007cited by this paper
• Structure of the multidrug ABC transporter Sav1866 from Staphylococcus aureus in complex with AMP‐PNP

  2007influential reference
• P-glycoprotein in the placenta: expression, localization, regulation and function.

  2006cited by this paper
• Conformational and functional characterization of trapped complexes of the P-glycoprotein multidrug transporter.

  2006cited by this paper
• Quantification and characterization of P-glycoprotein-substrate interactions.

  2006cited by this paper
• Drug resistance: Passing on protection

  2005cited by this paper
• Resolution of two substrate-binding sites in an engineered cytochrome P450eryF bearing a fluorescent probe.

  2005cited by this paper
• Direct observation of ligand binding to membrane proteins in living cells by a saturation transfer double difference (STDD) NMR spectroscopy method shows a significantly higher affinity of integrin alpha(IIb)beta3 in native platelets than in liposomes.

  2005cited by this paper
• Improved energy coupling of human P-glycoprotein by the glycine 185 to valine mutation.

  2004cited by this paper
• Pharmacogenomics of heart failure -- focus on drug disposition and action.

  2004cited by this paper
• Stoichiometry and affinity of nucleotide binding to P-glycoprotein during the catalytic cycle.

  2003cited by this paper
• New insights into the bioenergetics of mitochondrial disorders using intracellular ATP reporters.

  2003cited by this paper
• The Role of P-glycoprotein in the Blood-Brain Barrier

  2003cited by this paper
• Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.

  2003cited by this paper
• Three-dimensional Structures of the Mammalian Multidrug Resistance P-glycoprotein Demonstrate Major Conformational Changes in the Transmembrane Domains upon Nucleotide Binding*

  2003cited by this paper
• Extracellular ATP as a signaling molecule for epithelial cells.

  2003cited by this paper
• Drug Binding in Human P-glycoprotein Causes Conformational Changes in Both Nucleotide-binding Domains*

  2003cited by this paper
• Fluorescence Techniques for Studying Membrane Transport Proteins

  2003cited by this paper
• Simultaneous Binding of Two Different Drugs in the Binding Pocket of the Human Multidrug Resistance P-glycoprotein*

  2003cited by this paper
• Fluorescence techniques for studying membrane transport proteins: the P-glycoprotein multidrug transporter.

  2003cited by this paper
• Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs.

  2003cited by this paper
• Permanent Activation of the Human P-glycoprotein by Covalent Modification of a Residue in the Drug-binding Site*

  2003cited by this paper
• Substrate-induced Conformational Changes in the Transmembrane Segments of Human P-glycoprotein

  2003cited by this paper
• Measurements of ATP in mammalian cells.

  2002cited by this paper
• Expression and Localization of P-glycoprotein in Human Heart

  2002cited by this paper
• What Determines the Intracellular ATP Concentration

  2002cited by this paper
• A Novel Electron Paramagnetic Resonance Approach to Determine the Mechanism of Drug Transport by P-glycoprotein*

  2002cited by this paper
• Correlation between Steady-state ATP Hydrolysis and Vanadate-induced ADP Trapping in Human P-glycoprotein

  2001cited by this paper
• Group epitope mapping by saturation transfer difference NMR to identify segments of a ligand in direct contact with a protein receptor.

  2001cited by this paper
• P-Glycoprotein conformational changes detected by antibody competition.

  2001cited by this paper
• Intrinsic fluorescence of the P-glycoprotein multidrug transporter: sensitivity of tryptophan residues to binding of drugs and nucleotides.

  2000influential reference
• Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein.

  2000cited by this paper
• A Novel Method for Measurement of Submembrane ATP Concentration*

  2000cited by this paper
• Glucose generates sub-plasma membrane ATP microdomains in single islet beta-cells. Potential role for strategically located mitochondria.

  1999cited by this paper
• Ligand-mediated Tertiary Structure Changes of Reconstituted P-glycoprotein

  1999influential reference
• Interaction of the P-glycoprotein multidrug transporter (MDR1) with high affinity peptide chemosensitizers in isolated membranes, reconstituted systems, and intact cells.

  1999cited by this paper
• Both ATP sites of human P-glycoprotein are essential but not symmetric.

  1999cited by this paper
• What students must know about the determination of enzyme kinetic parameters

  1999cited by this paper
• Insights into the structure and substrate interactions of the P-glycoprotein multidrug transporter from spectroscopic studies.

  1999cited by this paper
• Large Scale Purification of Detergent-soluble P-glycoprotein fromPichia pastoris Cells and Characterization of Nucleotide Binding Properties of Wild-type, Walker A, and Walker B Mutant Proteins*

  1999cited by this paper
• Contribution to substrate specificity and transport of nonconserved residues in transmembrane domain 12 of human P-glycoprotein.

  1998cited by this paper
• Dissection of drug-binding-induced conformational changes in P-glycoprotein.

  1998cited by this paper
• Radioligand-Binding Assay Employing P-Glycoprotein-Overexpressing Cells: Testing Drug Affinities to the Secretory Intestinal Multidrug Transporter

  1998cited by this paper
• Drug-stimulated ATPase Activity of Human P-glycoprotein Requires Movement between Transmembrane Segments 6 and 12*

  1997cited by this paper
• Competitive, non-competitive and cooperative interactions between substrates of P-glycoprotein as measured by its ATPase activity.

  1997cited by this paper
• ATPase activity of P-glycoprotein related to emergence of drug resistance in Ehrlich ascites tumor cell lines.

  1997cited by this paper
• Intracellular Adenosine Triphosphate (ATP) Concentration: A Switch in the Decision Between Apoptosis and Necrosis

  1997cited by this paper
• Disadvantages of double reciprocal plots

  1997cited by this paper
• Structure-activity relationships of P-glycoprotein interacting drugs: kinetic characterization of their effects on ATPase activity.

  1997cited by this paper
• Inhibition of Oxidative Cross-linking between Engineered Cysteine Residues at Positions 332 in Predicted Transmembrane Segments (TM) 6 and 975 in Predicted TM12 of Human P-glycoprotein by Drug Substrates*

  1996cited by this paper
• Functional characterization of a glycine 185-to-valine substitution in human P-glycoprotein by using a vaccinia-based transient expression system.

  1996cited by this paper
• Effects of steroids and verapamil on P-glycoprotein ATPase activity: progesterone, desoxycorticosterone, corticosterone and verapamil are mutually non-exclusive modulators.

  1996cited by this paper
• Competition of Hydrophobic Peptides, Cytotoxic Drugs, and Chemosensitizers on a Common P-glycoprotein Pharmacophore as Revealed by Its ATPase Activity (*)

  1996cited by this paper
• Characterization of the ATPase activity of P-glycoprotein from multidrug-resistant Chinese hamster ovary cells.

  1995cited by this paper
• Functional Dissection of P-glycoprotein Nucleotide-binding Domains in Chimeric and Mutant Proteins

  1995cited by this paper
• Mutation of glycine 185 to valine alters the ATPase function of the human P-glycoprotein expressed in Sf9 cells.

  1995cited by this paper
• Both P-glycoprotein Nucleotide-binding Sites Are Catalytically Active (*)

  1995cited by this paper
• Adenosine 5'-(gamma-thiotriphosphate): an ATP analog that should be used with caution in muscle contraction studies.

  1995cited by this paper
• Drug-stimulated ATPase activity of a deletion mutant of the human multidrug-resistance protein (MDR1).

  1995cited by this paper
• MDR expression in normal tissues. Pharmacologic implications for the clinical use of P-glycoprotein inhibitors.

  1995cited by this paper
• Effects of lipids on ATPase activity of purified Chinese hamster P-glycoprotein.

  1995cited by this paper
• ATPase activity of purified and reconstituted P-glycoprotein from Chinese hamster ovary cells.

  1994cited by this paper
• Characterization of the ATPase activity of purified Chinese hamster P-glycoprotein.

  1994cited by this paper
• Interaction of calcium channel antagonists with calcium: structural studies on verapamil and its Ca2+ complex.

  1993cited by this paper
• Gradient-tailored excitation for single-quantum NMR spectroscopy of aqueous solutions

  1992cited by this paper
• Skeletal muscle metabolism in the chronic fatigue syndrome. In vivo assessment by 31P nuclear magnetic resonance spectroscopy.

  1992cited by this paper
• Partial purification and reconstitution of the human multidrug-resistance pump: characterization of the drug-stimulatable ATP hydrolysis.

  1992cited by this paper
• Nuclear magnetic resonance investigations of calcium antagonist drugs. II: Conformational and dynamic features of verapamil in [2H6]DMSO.

  1991cited by this paper
• Using linear and non-linear regression to fit biochemical data.

  1990cited by this paper
• A method for the determination of inorganic phosphate in the presence of labile organic phosphate and high concentrations of protein: application to lens ATPases.

  1988cited by this paper
• ATP and the regulation of renal cell function.

  1986cited by this paper
• Principles of fluorescence spectroscopy

  1983influential reference

• Research Progress on the Mechanisms of Action, Pharmacological Activities and Clinical Application of P-glycoprotein Inhibitors.

  2026cites this paper
• Drug-bound P-glycoprotein reveals nucleotide-dependent ligand pockets and ingress channels

  2025influential citation
• Outward-facing P-glycoprotein bound to drug displays nucleotide-dependent drug egress mechanism

  2025influential citation
• Assessment of Intramuscular Verapamil as Pharmacological Countermeasure in a Rat Model of Organophosphate DFP-induced Status Epilepticus

  2025cites this paper
• Mechanistic insights into P-glycoprotein-driven transport of anti-cancer PARP inhibitors.

  2025cites this paper
• Elucidating the Complex Structural and Molecular Mechanisms Driving P-Glycoprotein-Mediated Transport of Cardiac Glycosides

  2025influential citation
• Harnessing cell cycle intervention and evading P-glycoprotein efflux: natural product-inspired C2-aminophenyl chromones as dual modulators against multidrug-resistant cancer.

  2025cites this paper
• Assessment of pharmacokinetics, safety, and neuroprotective efficacy of an adjunct intramuscular verapamil therapy in a rat model of organophosphate DFP-induced status epilepticus

  2025cites this paper
• Selective Inhibition of the ABCG2 Transporter by Primaquine Derivatives Reverses the Multidrug Resistance of Tumor Cells

  2025cites this paper
• Verapamil and its metabolite norverapamil inhibit the Mycobacterium tuberculosis MmpS5L5 efflux pump to increase bedaquiline activity

  2025cites this paper
• Insights into interactions between taxanes and P-glycoprotein using biophysical and in silico methods.

  2025cites this paper
• Cryo-EM of human P-glycoprotein reveals an intermediate occluded conformation during active drug transport

  2025cites this paper
• Tolerability of tariquidar - A third generation P-gp inhibitor as add-on medication to antiseizure medications in drug-resistant epilepsy.

  2024cites this paper
• PROTAC-attractive site as a new target for suppressing P-glycoprotein activity.

  2024cites this paper
• Progress in Research of Nanotherapeutics for Overcoming Multidrug Resistance in Cancer

  2024cites this paper
• Utilizing surface plasmon resonance as a novel method for monitoring in-vitro P-glycoprotein efflux

  2024influential citation
• The human proton pump inhibitors inhibit Mycobacterium tuberculosis rifampicin efflux and macrophage-induced rifampicin tolerance

  2023cites this paper
• Vitexin along with verapamil downregulates efflux pump P-glycoprotein in macrophages and potentiate M1 to M2 switching via TLR4-NF-κB-TNFR2 pathway in lipopolysaccharide treated mice.

  2023cites this paper
• Genetics of ABCB1 in Cancer

  2023cites this paper
• Advantages and potential limitations of applying AFM kymograph analysis to pharmaceutically relevant membrane proteins in lipid bilayers

  2023cites this paper
• Coleon U, Isolated from Plectranthus mutabilis Codd., Decreases P-Glycoprotein Activity Due to Mitochondrial Inhibition

  2023cites this paper
• Interaction of a Homologous Series of Amphiphiles with P-glycoprotein in a Membrane Environment—Contributions of Polar and Non-Polar Interactions

  2023cites this paper
• Targeting the two-pore channel 2 in cancer progression and metastasis

  2022cites this paper
• Hijacking the intrinsic vitamin B12 pathway for the oral delivery of nanoparticles, resulting in enhanced in vivo anti-leishmanial activity.

  2022cites this paper
• Novel Sigma-2 receptor ligand A011 overcomes MDR in adriamycin-resistant human breast cancer cells by modulating ABCB1 and ABCG2 transporter function

  2022cites this paper
• The History of the ABC Proteins in Human Trypanosomiasis Pathogens

  2022influential citation
• Flavonoids as P-glycoprotein inhibitors for multidrug resistance in cancer: an in-silico approach

  2022influential citation
• Human gut Actinobacteria boost drug absorption by secreting P-glycoprotein ATPase inhibitors

  2022influential citation
• Four Decades of Cytochrome P450 2B Research: From Protein Adducts to Protein Structures and Beyond

  2022cites this paper
• Sensitizing multidrug-resistant leukemia cells to common cytostatics by an aluminium-salen complex that has high-apoptotic effects in leukemia, lymphoma and mamma carcinoma cells

  2021cites this paper
• Microplastics boost the accumulation of tetrabromobisphenol A in a commercial clam and elevate corresponding food safety risks.

  2021cites this paper
• Exploring new Horizons in overcoming P-glycoprotein-mediated multidrug-resistant breast cancer via nanoscale drug delivery platforms

  2021cites this paper
• Effect of the Force Field on Molecular Dynamics Simulations of the Multidrug Efflux Protein P-Glycoprotein.

  2021cites this paper
• The Use of Antihypertensive Drugs as Coadjuvant Therapy in Cancer

  2021cites this paper
• Acquired Drug Resistance Enhances Imidazoquinoline Efflux by P-Glycoprotein

  2021cites this paper
• Remodelling structure-based drug design using machine learning.

  2021cites this paper
• Overexpression of ABCB1 Transporter Confers Resistance to mTOR Inhibitor WYE-354 in Cancer Cells

  2020cites this paper
• The Intestinal Efflux Transporter Inhibition Activity of Xanthones from Mangosteen Pericarp: An In Silico, In Vitro and Ex Vivo Approach

  2020cites this paper
• Conformational changes in the nucleotide‐binding domains of P‐glycoprotein induced by ATP hydrolysis

  2020cites this paper
• Nanoparticle delivery of a pH-sensitive prodrug of doxorubicin and a mitochondrial targeting VES-H8R8 synergistically kill multi-drug resistant breast cancer cells

  2020cites this paper
• miRNA-29a reverses P-glycoprotein-mediated drug resistance and inhibits proliferation via up-regulation of PTEN in colon cancer cells.

  2020cites this paper
• Hsp90 facilitates acquired drug resistance of tumor cells through cholesterol modulation however independent of tumor progression.

  2020cites this paper
• The effects of anthracycline drugs on the conformational distribution of mouse P-glycoprotein explains their transport rate differences.

  2020influential citation
• Synergistic Nanoparticle Formulations against Multi-drug Resistant Breast Cancers

  2019cites this paper
• Incorporation of drug efflux inhibitor and chemotherapeutic agent into an inorganic/organic platform for the effective treatment of multidrug resistant breast cancer

  2019cites this paper
• Prediction of Drug Permeability Using In Vitro Blood–Brain Barrier Models with Human Induced Pluripotent Stem Cell-Derived Brain Microvascular Endothelial Cells

  2019cites this paper
• Cloud Point Extraction Combined with Liquid Chromatography Coupled to Tandem Mass Spectrometry for the Determination of Verapamil in Urine

  2019cites this paper
• Cationic block amphiphiles show anti-mitochondrial activity in multi-drug resistant breast cancer cells.

  2019cites this paper
• An Energetically Favorable Ligand Entrance Gate of a Multidrug Transporter Revealed by Partial Nudged Elastic Band Simulations

  2019cites this paper
• Evaluation of Intestinal Absorption and Bioavailability of a Bergenin–Phospholipid Complex Solid Dispersion in Rats

  2018cites this paper
• substrate transport upon cooperative estradiol-17-ß-D-3 glucuronide binding in a Drosophila ABCC transporter 4 5 Short title : 6 Increased coupling by cooperative substrate binding in Drosophila ABCC

  2018influential citation
• A Conformationally Gated Model of Methadone and Loperamide Transport by P-Glycoprotein.

  2018cites this paper
• The reliability of molecular dynamics simulations of the multidrug transporter P-glycoprotein in a membrane environment

  2018cites this paper
• The conformation and dynamics of P‐glycoprotein in a lipid bilayer investigated by atomic force microscopy

  2018cites this paper
• Differential Coupling of Binding, ATP Hydrolysis, and Transport of Fluorescent Probes with P-Glycoprotein in Lipid Nanodiscs.

  2017cites this paper
• Exploring Jolkinol D Derivatives To Overcome Multidrug Resistance in Cancer.

  2017cites this paper
• Boosted coupling of ATP hydrolysis to substrate transport upon cooperative estradiol‐17‐β‐D‐glucuronide binding in a Drosophila ATP binding cassette type‐C transporter

  2017cites this paper
• Insights Into the Molecular Mechanism of Triptan Transport by P-glycoprotein.

  2017cites this paper