Transition state P-glycoprotein binds drugs and modulators with unchanged affinity, suggesting a concerted transport mechanism.

No abstract is available for this paper.

• Publication year

  2003

• Venue

  Biochemistry

• Publication date

  2003-01-17

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/BI0267745PMID 12564938
• 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.

• Mechanisms of cancer drug resistance.

  2002cited by this paper
• Vanadate-catalyzed photocleavage of the signature motif of an ATP-binding cassette (ABC) transporter

  2002cited by this paper
• Structural and Functional Asymmetry of the Nucleotide-binding Domains of P-glycoprotein Investigated by Attenuated Total Reflection Fourier Transform Infrared Spectroscopy*

  2002cited by this paper
• Overview: ABC Transporters and Human Disease

  2001cited by this paper
• Phospholipid flippase activity of the reconstituted P-glycoprotein multidrug transporter.

  2001cited by this paper
• Cysteines 431 and 1074 Are Responsible for Inhibitory Disulfide Cross-linking between the Two Nucleotide-binding Sites in Human P-glycoprotein*

  2001cited by this paper
• Characterization of the Catalytic Cycle of ATP Hydrolysis by Human P-glycoprotein

  2001cited by this paper
• FRET analysis indicates that the two ATPase active sites of the P-glycoprotein multidrug transporter are closely associated.

  2001cited by this paper
• Drug transport by reconstituted P-glycoprotein in proteoliposomes. Effect of substrates and modulators, and dependence on bilayer phase state.

  2001cited by this paper
• Complete Characterization of the Human ABC Gene Family

  2001cited by this paper
• The Arabidopsis thaliana ABC Protein Superfamily, a Complete Inventory*

  2001cited by this paper
• From MDR to MXR: new understanding of multidrug resistance systems, their properties and clinical significance

  2001cited by this paper
• Fungal ABC proteins: pleiotropic drug resistance, stress response and cellular detoxification.

  2001cited by this paper
• Structure of MsbA from E. coli: a homolog of the multidrug resistance ATP binding cassette (ABC) transporters.

  2001cited by this paper
• The vinblastine binding site adopts high- and low-affinity conformations during a transport cycle of P-glycoprotein.

  2001cited by this paper
• The Mechanism of Action of Multidrug-Resistance-Linked P-Glycoprotein

  2001cited by this paper
• The ABC of ABCS: a phylogenetic and functional classification of ABC systems in living organisms.

  2001cited by this paper
• ABC transporters: physiology, structure and mechanism--an overview.

  2001cited by this paper
• Exploring the structure and function of the P-glycoprotein multidrug transporter using fluorescence spectroscopic tools.

  2001cited by this paper
• Trapping the transition state of an ATP-binding cassette transporter: evidence for a concerted mechanism of maltose transport.

  2001cited by this paper
• The Role of Half-Transporters in Multidrug Resistance

  2001cited by this paper
• Repacking of the transmembrane domains of P‐glycoprotein during the transport ATPase cycle

  2001cited by this paper
• Analysis of MDR1 P-glycoprotein conformational changes in permeabilized cells using differential immunoreactivity.

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

  2000cited by this paper
• Molecular Properties of Bacterial Multidrug Transporters

  2000cited by this paper
• Antibiotic resistance: era of the multidrug pump

  2000cited by this paper
• Structural biology of Rad50 ATPase: ATP-driven conformational control in DNA double-strand break repair and the ABC-ATPase superfamily.

  2000cited by this paper
• Evidence for a requirement for ATP hydrolysis at two distinct steps during a single turnover of the catalytic cycle of human P-glycoprotein.

  2000cited by this paper
• The homodimeric ATP‐binding cassette transporter LmrA mediates multidrug transport by an alternating two‐site (two‐cylinder engine) mechanism

  2000cited by this paper
• Nucleotide-induced conformational changes in P-glycoprotein and in nucleotide binding site mutants monitored by trypsin sensitivity.

  2000cited by this paper
• Vanadate-Induced Trapping of Nucleotides by Purified Maltose Transport Complex Requires ATP Hydrolysis

  2000cited by this paper
• Biochemical, cellular, and pharmacological aspects of the multidrug transporter.

  1999cited by this paper
• Characterization of binding properties to human P-glycoprotein: development of a [3H]verapamil radioligand-binding assay.

  1999cited by this paper
• Getting In or Out: Early Segregation Between Importers and Exporters in the Evolution of ATP-Binding Cassette (ABC) Transporters

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

  1999cited by this paper
• ABC-ATPases, adaptable energy generators fuelling transmembrane movement of a variety of molecules in organisms from bacteria to humans.

  1999cited by this paper
• Subunit interactions in ABC transporters: towards a functional architecture.

  1999cited by this paper
• The membrane lipid environment modulates drug interactions with the P-glycoprotein multidrug transporter.

  1999cited by this paper
• Human P-glycoprotein exhibits reduced affinity for substrates during a catalytic transition state.

  1998cited by this paper
• The Escherichia coli ATP‐binding cassette (ABC) proteins

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

  1998cited by this paper
• Linear and cyclic peptides as substrates and modulators of P-glycoprotein: peptide binding and effects on drug transport and accumulation.

  1998cited by this paper
• ATP-binding-cassette (ABC) transport systems: functional and structural aspects of the ATP-hydrolyzing subunits/domains.

  1998cited by this paper
• Extraction of Hoechst 33342 from the cytoplasmic leaflet of the plasma membrane by P-glycoprotein.

  1997cited by this paper
• P-glycoprotein-mediated Hoechst 33342 transport out of the lipid bilayer.

  1997cited by this paper
• The P-Glycoprotein Efflux Pump: How Does it Transport Drugs?

  1997cited by this paper
• Fluorescence studies on the nucleotide binding domains of the P-glycoprotein multidrug transporter.

  1997cited by this paper
• X-ray structure of the magnesium(II).ADP.vanadate complex of the Dictyostelium discoideum myosin motor domain to 1.9 A resolution.

  1996cited by this paper
• Synthetic hydrophobic peptides are substrates for P-glycoprotein and stimulate drug transport.

  1996cited by this paper
• Site-directed fluorescence labeling of P-glycoprotein on cysteine residues in the nucleotide binding domains.

  1996cited by this paper
• The catalytic cycle of P‐glycoprotein

  1995cited by this paper
• Covalent Modification of Human P-glycoprotein Mutants Containing a Single Cysteine in Either Nucleotide-binding Fold Abolishes Drug-stimulated ATPase Activity (*)

  1995cited by this paper
• Interaction of the P-glycoprotein Multidrug Transporter with Peptides and Ionophores (*)

  1995cited by this paper
• Characterization of the ATPase activity of P-glycoprotein from multidrug-resistant Chinese hamster ovary cells.

  1995cited by this paper
• P-glycoprotein Is Stably Inhibited by Vanadate-induced Trapping of Nucleotide at a Single Catalytic Site (*)

  1995cited by this paper
• Interaction of multidrug-resistant Chinese hamster ovary cells with the peptide ionophore gramicidin D.

  1994cited by this paper
• Functional reconstitution of drug transport and ATPase activity in proteoliposomes containing partially purified P-glycoprotein.

  1993cited by this paper
• ATPase activity of partially purified P-glycoprotein from multidrug-resistant Chinese hamster ovary cells.

  1992cited by this paper
• Is the multidrug transporter a flippase?

  1992cited by this paper
• Photocleavage of myosin subfragment 1 by vanadate.

  1990cited by this paper
• Vesicles of variable sizes produced by a rapid extrusion procedure.

  1986cited by this paper
• Uptake of antineoplastic agents into large unilamellar vesicles in response to a membrane potential.

  1985cited by this paper
• A simplification of the protein assay method of Lowry et al. which is more generally applicable.

  1977cited by this paper

• Vinca alkaloid binding to P-glycoprotein occurs in a processive manner.

  2022cites this paper
• Effects of cholesterol content on activity of P-glycoproteins and membrane physical state, and consequences for anthelmintic resistance in the nematode Haemonchus contortus

  2020cites this paper
• New Evidence for P-gp-Mediated Export of Amyloid-β Peptides in Molecular, Blood-Brain Barrier and Neuronal Models

  2020cites this paper
• Antitumour Anthracyclines: Progress and Perspectives

  2020cites this paper
• Differential Coupling of Binding, ATP Hydrolysis, and Transport of Fluorescent Probes with P-Glycoprotein in Lipid Nanodiscs.

  2017cites this paper
• Identification of the Distance between the Homologous Halves of P-glycoprotein That Triggers the High/Low ATPase Activity Switch*

  2014cites this paper
• Tariquidar inhibits P-glycoprotein drug efflux but activates ATPase activity by blocking transition to an open conformation.

  2014cites this paper
• Kinetic Validation of the Models for P-Glycoprotein ATP Hydrolysis and Vanadate-Induced Trapping. Proposal for Additional Steps

  2014cites this paper
• The Cross-Talk between Canonical and Non-Canonical Wnt-Dependent Pathways Regulates P-Glycoprotein Expression in Human Blood–Brain Barrier Cells

  2014cites this paper
• Mammalian P4-ATPases and ABC transporters and their role in phospholipid transport.

  2013cites this paper
• Perspectives on the structure-function of ABC transporters: the Switch and Constant Contact models.

  2012cites this paper
• Dynamic Ligand-induced Conformational Rearrangements in P-glycoprotein as Probed by Fluorescence Resonance Energy Transfer Spectroscopy*

  2011cites this paper
• Catalytic and transport cycles of ABC exporters.

  2011cites this paper
• Fluorescence studies of drug binding and translocation by membrane transporters.

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

  2010cites this paper
• Uncoupling Substrate Transport from ATP Hydrolysis in the Escherichia coli Maltose Transporter*

  2010cites this paper
• Translation of novel anti-cancer cytotoxicity biomarkers detected with high content analysis from an in vitro predictive model to an in vivo cell model.

  2010cites this paper
• Multidrug resistance through the spectacle of P-glycoprotein.

  2009cites this paper
• Molecular basis of multidrug transport by ABC transporters.

  2009cites this paper
• ABC efflux pump-based resistance to chemotherapy drugs.

  2009cites this paper
• Multidrug Resistance Protein ( P-Glycoprotein ; MDR 1 )

  2009cites this paper
• CLC-0 and CFTR: chloride channels evolved from transporters.

  2008cites this paper
• P-glycoprotein senses its substrates and the lateral membrane packing density: consequences for the catalytic cycle.

  2008cites this paper
• Chalcogenopyrylium dyes as inhibitors/modulators of P-glycoprotein in multidrug-resistant cells.

  2008cites this paper
• P-Glycoprotein in Proteoliposomes with Low Residual Detergent: The Effects of Cholesterol

  2007cites this paper
• Catalytic cycle of ATP hydrolysis by P-glycoprotein: evidence for formation of the E.S reaction intermediate with ATP-gamma-S, a nonhydrolyzable analogue of ATP.

  2007cites this paper
• The Walker B motif of the second nucleotide-binding domain (NBD2) of CFTR plays a key role in ATPase activity by the NBD1-NBD2 heterodimer.

  2007cites this paper
• About a switch: how P-glycoprotein (ABCB1) harnesses the energy of ATP binding and hydrolysis to do mechanical work

  2007cites this paper
• Synergy between verapamil and other multidrug-resistance modulators in model membranes

  2007cites this paper
• Stimulation of P-glycoprotein ATPase by analogues of tetramethylrosamine: coupling of drug binding at the "R" site to the ATP hydrolysis transition state.

  2006cites this paper
• Defense System Transporters: Participation in a Chemoimmunity Human Multidrug Resistance ABCB and ABCG

  2006cites this paper
• P-glycoprotein-reconstitution into liposomes to study the influence of the lipid bilayer composition on its function

  2006cites this paper
• Exploiting Reaction Intermediates of the ATPase Reaction to Elucidate the Mechanism of Transport by P-glycoprotein (ABCB1)*

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

  2006cites this paper
• Human multidrug resistance ABCB and ABCG transporters: participation in a chemoimmunity defense system.

  2006cites this paper
• Shedding light on drug transport: structure and function of the P-glycoprotein multidrug transporter (ABCB1).

  2006cites this paper
• Recent Progress in Understanding the Mechanism of P-Glycoprotein-mediated Drug Efflux

  2005cites this paper
• Interaction of LDS-751 and rhodamine 123 with P-glycoprotein: evidence for simultaneous binding of both drugs.

  2005cites this paper
• Interaction of LDS-751 with P-glycoprotein and mapping of the location of the R drug binding site.

  2005cites this paper
• Increased resistance to anthelmintics of Haemonchus contortus eggs associated with changes in membrane fluidity of eggshells during embryonation

  2005cites this paper
• The elementary mass action rate constants of P-gp transport for a confluent monolayer of MDCKII-hMDR1 cells.

  2005cites this paper
• The Steady-State Michaelis–Menten Analysis of P-Glycoprotein Mediated Transport Through a Confluent Cell Monolayer Cannot Predict the Correct Michaelis Constant Km

  2005cites this paper
• New Insights into the Drug Binding, Transport and Lipid Flippase Activities of the P-Glycoprotein Multidrug Transporter

  2005cites this paper
• ATP-sensitive K+ channel channel/enzyme multimer: metabolic gating in the heart.

  2005cites this paper
• Discrimination of live and early apoptotic mononuclear cells by the fluorescent SYTO 16 vital dye.

  2005cites this paper
• The ATP switch model for ABC transporters

  2004cites this paper
• Reversible Transport by the ATP-binding Cassette Multidrug Export Pump LmrA

  2004cites this paper
• The ABC transporter structure and mechanism: perspectives on recent research

  2004cites this paper
• ATP-binding cassette transporters in bacteria.

  2004cites this paper
• Energetics of wild-type and mutant multidrug resistance secondary transporter LmrP of Lactococcus lactis.

  2004cites this paper
• Functional evaluation of ABCB1 (P-glycoprotein) polymorphisms: high-speed screening and structure-activity relationship analyses.

  2004cites this paper
• Drug efflux mechanism by a secondary transporter LmrP of Lactococcus lactis

  2004cites this paper
• How do ABC transporters drive transport?

  2004cites this paper
• University of Groningen Energetics of wild-type and mutant multidrug resistance secondary transporter LmrP of Lactococcus lactis Mazurkiewicz,

  2004cites this paper
• Pharmacogenomics of drug transporters: a new approach to functional analysis of the genetic polymorphisms of ABCB1 (P-glycoprotein/MDR1).

  2004cites this paper
• Conformational Transitions Induced by the Binding of MgATP to the Vitamin B12 ATP-binding Cassette (ABC) Transporter BtuCD*

  2004cites this paper
• Transition State Analysis of the Coupling of Drug Transport to ATP Hydrolysis by P-glycoprotein*

  2003cites this paper
• Acidic Residues in the Lactococcal Multidrug Efflux Pump LmrP Play Critical Roles in Transport of Lipophilic Cationic Compounds*

  2002cites this paper