Clinical Relevance of P-Glycoprotein in Drug Therapy

Death Receptors: Signaling and Modulation

1998 • 5,873 citations

The Bcl-2 Protein Family: Arbiters of Cell Survival

1998 • 5,359 citations

Multidrug resistance in cancer: role of ATP–dependent transporters

2002 • 5,195 citations

A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants

1976 • 3,228 citations

Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues.

1987 • 2,788 citations

Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs

1994 • 2,255 citations

Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells

1991 • 1,787 citations

Multidrug-resistance gene (P-glycoprotein) is expressed by endothelial cells at blood-brain barrier sites.

1989 • 1,744 citations

A Matter of Life and Cell Death

1998 • 1,523 citations

Caco-2 monolayers in experimental and theoretical predictions of drug transport1PII of original article: S0169-409X(96)00415-2. The article was originally published in Advanced Drug Delivery Reviews 22 (1996) 67–84.1

2001 • 1,479 citations

Overcoming of vincristine resistance in P388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil.

1981 • 1,463 citations

P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs.

1996 • 1,268 citations

Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A.

1995 • 1,109 citations

Expression of the multidrug resistance gene product (P-glycoprotein) in human normal and tumor tissues.

1990 • 1,063 citations

The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors.

1998 • 1,058 citations

Normal viability and altered pharmacokinetics in mice lacking mdr1-type (drug-transporting) P-glycoproteins

1997 • 934 citations

Detection of P-glycoprotein in multidrug-resistant cell lines by monoclonal antibodies

1985 • 927 citations

The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin

1999 • 911 citations

Role of P-Glycoprotein in Pharmacokinetics

2003 • 897 citations

MDCK (Madin-Darby Canine Kidney) Cells: A Tool for Membrane Permeability Screening

1999 • 895 citations

Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine

1997 • 871 citations

Relationship of octanol/water partition coefficient and molecular weight to rat brain capillary permeability

1980 • 799 citations

Pharmacological characterization of multidrug resistant MRP-transfected human tumor cells.

1994 • 777 citations

Paclitaxel-resistant Human Ovarian Cancer Cells Have Mutant β-Tubulins That Exhibit Impaired Paclitaxel-driven Polymerization

1997 • 668 citations

Rational use of in vitro P-glycoprotein assays in drug discovery.

2001 • 637 citations

Immunohistochemical localization in normal tissues of different epitopes in the multidrug transport protein P170: evidence for localization in brain capillaries and crossreactivity of one antibody with a muscle protein.

1989 • 606 citations

Passive Permeability and P-Glycoprotein-Mediated Efflux Differentiate Central Nervous System (CNS) and Non-CNS Marketed Drugs

2002 • 590 citations

Mechanisms of Action of and Resistance to Antitubulin Agents: Microtubule Dynamics, Drug Transport, and Cell Death

1999 • 579 citations

Choroid plexus epithelial expression of MDR 1 P glycoprotein and multidrug resistance-associated protein contribute to the blood–cerebrospinal-fluid drug-permeability barrier

1999 • 529 citations

Overexpression of the BCRP/MXR/ABCP gene in a topotecan-selected ovarian tumor cell line.

1999 • 475 citations

Active efflux of daunorubicin and adriamycin in sensitive and resistant sublines of P388 leukemia.

1979 • 454 citations

Transport of Protein-Bound Hormones into Tissuesin Vivo*

1981 • 435 citations

Acquired mutations in the MXR/BCRP/ABCP gene alter substrate specificity in MXR/BCRP/ABCP-overexpressing cells.

2001 • 427 citations

Verapamil and adriamycin in the treatment of drug-resistant ovarian cancer patients.

1987 • 425 citations

Increased drug delivery to the brain by P-glycoprotein inhibition

2000 • 422 citations

Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole or itraconazole

1994 • 407 citations

Blood–Brain Barrier in Physiology and Medicine

1977 • 395 citations

Characterization of vincristine transport by the M(r) 190,000 multidrug resistance protein (MRP): evidence for cotransport with reduced glutathione.

1998 • 392 citations

Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.

2000 • 384 citations

Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells. Kinetics of vinblastine secretion and interaction with modulators

1993 • 365 citations

Transporter-Mediated Permeation of Drugs Across the Blood–Brain Barrier

2000 • 361 citations

Multidrug resistance protein 1 protects the choroid plexus epithelium and contributes to the blood-cerebrospinal fluid barrier

2000 • 358 citations

Clinical Pharmacokinetics and Pharmacodynamics of Cholinesterase Inhibitors

2002 • 348 citations

Is the role of the small intestine in first-pass metabolism overemphasized?

1999 • 344 citations

The cell biology of multiple drug resistance

1987 • 340 citations

Ceramide glycosylation potentiates cellular multidrug resistance

2001 • 303 citations

Alteration of etoposide pharmacokinetics and pharmacodynamics by cyclosporine in a phase I trial to modulate multidrug resistance.

1992 • 298 citations

Drug efflux transporters in the CNS

2003 • 295 citations

P-glycoprotein as the drug efflux pump in primary cultured bovine brain capillary endothelial cells

1992 • 288 citations

Gene amplification, drug resistance, and cancer.

1984 • 284 citations

Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: A new type of drug/drug interaction

2000 • 281 citations

Full blockade of intestinal P-glycoprotein and extensive inhibition of blood-brain barrier P-glycoprotein by oral treatment of mice with PSC833.

1997 • 272 citations

Caco-2 monolayers in experimental and theoretical predictions of drug transport

1996 • 268 citations

Mrp1 Multidrug Resistance‐Associated Protein and P‐Glycoprotein Expression in Rat Brain Microvessel Endothelial Cells

1998 • 265 citations

Direct correlation between DNA topoisomerase II activity and cytotoxicity in adriamycin-sensitive and -resistant P388 leukemia cell lines.

1989 • 263 citations

Verapamil

1989 • 254 citations

A morphometric study on the development of the lateral ventricle choroid plexus, choroid plexus capillaries and ventricular ependyma in the rat

1990 • 239 citations

Rifampin drastically reduces plasma concentrations and effects of oral midazolam

1996 • 238 citations

The drug efflux–metabolism alliance: biochemical aspects

2001 • 230 citations

In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results.

2001 • 226 citations

P-Glycoprotein Limits the Brain Penetration of Nonsedating but not Sedating H1-Antagonists

2003 • 225 citations

Oral Drug Absorption: Prediction and Assessment

2000 • 224 citations

Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers.

1993 • 217 citations

Role of P-glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor.

1999 • 216 citations

Protein Binding as a Primary Determinant of the Clinical Pharmacokinetic Properties of Non-Steroidal Anti-Inflammatory Drugs

1987 • 207 citations

Hydrogen bonding potential as a determinant of the in vitro and in situ blood-brain barrier permeability of peptides.

1994 • 201 citations

Intestinal drug metabolism and antitransport processes: A potential paradigm shift in oral drug delivery

1996 • 194 citations

Relative frequency and kinetic properties of transport-defective phenotypes among methotrexate-resistant L1210 clonal cell lines derived in vivo.

1981 • 191 citations

Estimation of the relative contribution of the transcellular and paracellular pathway to the transport of passively absorbed drugs in the Caco-2 cell culture model.

1997 • 188 citations

Complete in vivo reversal of P‐glycoprotein pump function in the blood‐brain barrier visualized with positron emission tomography

1998 • 182 citations

Phase I study of etoposide with SDZ PSC 833 as a modulator of multidrug resistance in patients with cancer.

1996 • 179 citations

Efflux transport systems for drugs at the blood–brain barrier and blood–cerebrospinal fluid barrier (Part 1)

2001 • 173 citations

Evidence for a Polarized Efflux System in Caco-2 Cells Capable of Modulating Cyclosporine A Transport

1993 • 167 citations

P‐glycoprotein‐mediated intestinal and biliary digoxin transport in humans

2003 • 156 citations

Thymidylate synthase overproduction and gene amplification in fluorodeoxyuridine-resistant human cells.

1985 • 154 citations

The prognostic significance of expression of the multidrug resistance-associated protein (MRP) in primary breast cancer

1997 • 151 citations

Phase I and pharmacokinetic study of paclitaxel in combination with biricodar, a novel agent that reverses multidrug resistance conferred by overexpression of both MDR1 and MRP.

1998 • 146 citations

Inhibitors of Multidrug Resistance to Antitumor Agents (MDR)

2002 • 145 citations

Taxol resistance mediated by transfection of the liver-specific sister gene of P-glycoprotein.

1998 • 144 citations

Evidence for a Polarized Efflux System for Peptides in the Apical Membrane of Caco-2 Cells

1993 • 141 citations

Increased accumulation of doxorubicin and doxorubicinol in cardiac tissue of mice lacking mdr1a P-glycoprotein

1998 • 141 citations

Multidrug Resistance‐Related Transport Proteins in Isolated Human Brain Microvessels and in Cells Cultured from These Isolates

1998 • 139 citations

Gene amplification in a leukemic patient treated with methotrexate.

1984 • 139 citations

Altered Expression of Mβ2, the Class II β-Tubulin Isotype, in a Murine J774.2 Cell Line with a High Level of Taxol Resistance

1995 • 138 citations

A new in vivo method to study P-glycoprotein transport in tumors and the blood-brain barrier.

1999 • 135 citations

Influence of P-glycoprotein on the transport and metabolism of indinavir in Caco-2 cells expressing cytochrome P-450 3A4.

2000 • 128 citations

Effect of Plasma Protein Binding on in Vivo Activity and Brain Penetration of Glycine/NMDA Receptor Antagonists

1997 • 128 citations

Considerations in the design and development of transport inhibitors as adjuncts to drug therapy

2003 • 128 citations

Uncoupling Ceramide Glycosylation by Transfection of Glucosylceramide Synthase Antisense Reverses Adriamycin Resistance

2000 • 127 citations

Cytologic evidence for gene amplification in methotrexate-resistant cells obtained from a patient with ovarian adenocarcinoma.

1984 • 123 citations

P-glycoprotein-dependent disposition kinetics of tacrolimus: studies in mdr1a knockout mice.

1999 • 113 citations

Evidence for intestinal secretion as an additional clearance pathway of talinolol enantiomers: concentration- and dose-dependent absorption in vitro and in vivo.

1996 • 112 citations

High levels of P-glycoprotein detected in isolated brain capillaries

1993 • 109 citations

Detection of in vivo P-glycoprotein inhibition by PSC 833 using Tc-99m sestamibi.

1997 • 104 citations

Expression and functional activity of P-glycoprotein in cultured cerebral capillary endothelial cells.

1992 • 99 citations

Intestinal secretion of intravenous talinolol is inhibited by luminal R-verapamil*

1999 • 95 citations

Clinical pharmacokinetics of doxorubicin in combination with GF120918, a potent inhibitor of MDR1 P-glycoprotein

1999 • 91 citations

Phase I Study of Infusional Paclitaxel in Combination With the P-Glycoprotein Antagonist PSC 833

2001 • 89 citations

Physiological pharmaceutics: biological barriers to drug absorption

1990 • 88 citations

A dose-finding and pharmacokinetic study of reversal of multidrug resistance with SDZ PSC 833 in combination with doxorubicin in patients with solid tumors.

1997 • 87 citations

Decreased retention of actinomycin D as the basis for cross-resistance in anthracycline-resistant sublines of P388 leukemia.

1977 • 87 citations

Development of Multidrug-Resistance Convertors: Sense or Nonsense?

2000 • 84 citations

Effect of ketoconazole on ritonavir and saquinavir concentrations in plasma and cerebrospinal fluid from patients infected with human immunodeficiency virus

2000 • 84 citations

Effect of dexamethasone on the intestinal first-pass metabolism of indinavir in rats: evidence of cytochrome P-450 3A [correction of P-450 A] and p-glycoprotein induction .

1999 • 83 citations

The Anatomic Basis of the Blood-Brain Barrier

1989 • 83 citations

Dipyridamole enhances digoxin bioavailability via P‐glycoprotein inhibition

2003 • 79 citations

Affinity for the P-Glycoprotein Efflux Pump at the Blood-Brain Barrier May Explain the Lack of CNS Side-Effects of Modern Antihistamines

2001 • 77 citations

Transepithelial transport of organic anions across the choroid plexus: possible involvement of organic anion transporter and multidrug resistance-associated protein.

1999 • 76 citations

Drug-protein binding and blood-brain barrier permeability.

1999 • 74 citations

Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro.

2000 • 74 citations

Efflux transport systems for drugs at the blood–brain barrier and blood–cerebrospinal fluid barrier (Part 2)

2001 • 74 citations

Mechanisms of multidrug resistance in human tumor cells. The roles of P-glycoprotein, DNA topoisomerase II, and other factors

1990 • 70 citations

Absolute quinidine bioavailability

1976 • 67 citations

Apparent lack of Mrp1-mediated efflux at the luminal side of mouse blood-brain barrier endothelial cells.

2003 • 66 citations

Longitudinal assessment of a P-glycoprotein?mediated drug interaction of valspodar on digoxin

1999 • 63 citations

Effect of heparin or salicylate infusion on serum protein binding and on concentrations of phenytoin in serum, brain and cerebrospinal fluid of rats.

1981 • 59 citations

Preclinical and Clinical Modulation of Anticancer Drugs

1993 • 58 citations

P-glycoprotein-mediated efflux of indinavir metabolites in Caco-2 cells expressing cytochrome P450 3A4.

2001 • 55 citations

Animal models for oral drug delivery in man : in situ and in vivo approaches

1983 • 53 citations

Apparent dose‐dependent oral absorption of cyclosporin a in rats

1984 • 49 citations

Steady-state pharmacokinetics of indinavir in cerebrospinal fluid and plasma among adults with human immunodeficiency virus type 1 infection

2000 • 42 citations

Effects of protein binding and experimental disease states on brain uptake of benzodiazepines in rats.

1990 • 42 citations

Effects of Ritonavir on Indinavir Pharmacokinetics in Cerebrospinal Fluid and Plasma

2003 • 41 citations

Defective facilitated diffusion of nucleosides, a primary mechanism of resistance to 5-fluoro-2'-deoxyuridine in the HCT-8 human carcinoma line.

1985 • 40 citations

MDR1 and multidrug resistance-associated protein (MRP) gene expression in epithelial ovarian tumors

1996 • 40 citations

Techniques for plasma protein binding of demethylchlorimipramine

1979 • 38 citations

MDR1 and MRP expression in chronic B‐cell lymphoproliferative disorders

1998 • 33 citations

Expression of the multidrug resistance-associated protein (MRP) gene in colorectal carcinomas

1997 • 33 citations

The expression of multidrug resistance protein in human gastrointestinal tract carcinomas

1998 • 32 citations

Expression of the multidrug resistance protein (MRP) in squamous cell carcinoma of the oesophagus and response to pre-operative chemotherapy

1998 • 28 citations

Interdependent Effect of P-Glycoprotein-Mediated Drug Efflux and Intracellular Drug Binding on Intracellular Paclitaxel Pharmacokinetics: Application of Computational Modeling

2003 • 17 citations

The Role of Brain Extracellular Fluid Production and Efflux Mechanisms in Drug Transport to the Brain

2000 • 14 citations

Cerebrospinal fluid production is normal in Down syndrome

1998 • 9 citations

Mathematical Models of Membrane Transport Processes

1978 • 4 citations