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Membrane transporters in drug development

Data up to Jan 2025

Published2010
Citations3,093
References219

Total Citations Per Year

Abstract

References (219)

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Substantial pharmacokinetic interaction between digoxin and ritonavir in healthy volunteers*1

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Sex-Dependent Expression and Activity of the ATP-Binding Cassette Transporter Breast Cancer Resistance Protein (BCRP/ABCG2) in Liver

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Impact of Genetic Polymorphisms of Transporters on the Pharmacokinetic, Pharmacodynamic and Toxicological Properties of Anionic Drugs

2008 • 162 citations

Drug/Drug Interaction Between Lopinavir/Ritonavir and Rosuvastatin in Healthy Volunteers

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Hepatic uptake of cholecystokinin octapeptide by organic anion-transporting polypeptides OATP4 and OATP8 of rat and human liver

2001 • 157 citations

Pharmacogenetic Characterization of Sulfasalazine Disposition Based on NAT2 and ABCG2 (BCRP) Gene Polymorphisms in Humans

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Scientific Perspectives on Drug Transporters and Their Role in Drug Interactions

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Species Difference in the Inhibitory Effect of Nonsteroidal Anti-Inflammatory Drugs on the Uptake of Methotrexate by Human Kidney Slices

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Breast Cancer Resistance Protein (Bcrp/abcg2) Is a Major Determinant of Sulfasalazine Absorption and Elimination in the Mouse

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Clinical Pharmacokinetics of Ranolazine

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Role of organic cation transporters in the renal handling of therapeutic agents and xenobiotics

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Physiology, structure, and regulation of the cloned organic anion transporters

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2007 • 122 citations

Overlapping in vitro and in vivo specificities of the organic anion transporters OAT1 and OAT3 for loop and thiazide diuretics

2008 • 122 citations

Methotrexate Pharmacokinetics in Transgenic Mice with Liver-Specific Expression of Human Organic Anion-Transporting Polypeptide 1B1 (SLCO1B1)

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A Global Drug Inhibition Pattern for the Human ATP-Binding Cassette Transporter Breast Cancer Resistance Protein (ABCG2)

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Organic cation transporters

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BCRP Transports Dipyridamole and is Inhibited by Calcium Channel Blockers

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Use of Tc-99m Mebrofenin as a Clinical Probe to Assess Altered Hepatobiliary Transport: Integration of In Vitro, Pharmacokinetic Modeling, and Simulation Studies

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A New Strategy of High-Speed Screening and Quantitative Structure-Activity Relationship Analysis to Evaluate Human ATP-Binding Cassette Transporter ABCG2-Drug Interactions

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Pharmacogenetics of SLCO1B1 gene and the impact of *1b and *15 haplotypes on irinotecan disposition in Asian cancer patients

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Investigation of the Inhibitory Effects of Various Drugs on the Hepatic Uptake of Fexofenadine in Humans

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Structural Variation Governs Substrate Specificity for Organic Anion Transporter (OAT) Homologs

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Effect of Human Renal Cationic Transporter Inhibition on the Pharmacokinetics of Varenicline, a New Therapy for Smoking Cessation: An In Vitro–In Vivo Study

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Differential Involvement of Mrp2 (Abcc2) and Bcrp (Abcg2) in Biliary Excretion of 4-Methylumbelliferyl Glucuronide and Sulfate in the Rat

2006 • 84 citations

Kidney-specific expression of human organic cation transporter 2 (OCT2/SLC22A2) is regulated by DNA methylation

2008 • 84 citations

Drug and toxicant handling by the OAT organic anion transporters in the kidney and other tissues

2007 • 80 citations

Drugdrug interactions involving membrane transporters in the human kidney

2006 • 79 citations

Unexpected Mexiletine Responses of a Mutant Cardiac Na+ Channel Implicate the Selectivity Filter as a Structural Determinant of Antiarrhythmic Drug Access

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A LC–MS/MS method to quantify the novel cholesterol lowering drug ezetimibe in human serum, urine and feces in healthy subjects genotyped for SLCO1B1

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Use of Sandwich-Cultured Human Hepatocytes to Predict Biliary Clearance of Angiotensin II Receptor Blockers and HMG-CoA Reductase Inhibitors

2008 • 72 citations

Vectorial Transport of the Peptide CCK-8 by Double-Transfected MDCKII Cells Stably Expressing the Organic Anion Transporter OATP1B3 (OATP8) and the Export Pump ABCC2

2005 • 71 citations

QSAR analysis and molecular modeling of ABCG2-specific inhibitors

2008 • 69 citations

Prediction of the Hepatic and Renal Clearance of Transporter Substrates in Rats Using in Vitro Uptake Experiments

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Pharmacogenomic importance of ABCG2

2008 • 69 citations

Effect of cimetidine and ranitidine on pharmacokinetics and pharmacodynamics of a single dose of dofetilide

2000 • 68 citations

Evaluation of the interaction between nonsteroidal anti-inflammatory drugs and methotrexate using human organic anion transporter 3-transfected cells

2008 • 68 citations

PhRMA White Paper on ADME Pharmacogenomics

2008 • 66 citations

Relationship between Drug/Metabolite Exposure and Impairment of Excretory Transport Function

2008 • 66 citations

Multichannel Liquid Chromatography–Tandem Mass Spectrometry Cocktail Method for Comprehensive Substrate Characterization of Multidrug Resistance-Associated Protein 4 Transporter

2007 • 65 citations

Human ABC Transporter ABCG2 in Xenobiotic Protection and Redox Biology

2006 • 64 citations

Predictors of Vinorelbine Pharmacokinetics and Pharmacodynamics in Patients With Cancer

2006 • 64 citations

Amino Acid Residues in Transmembrane Domain 10 of Organic Anion Transporting Polypeptide 1B3 Are Critical for Cholecystokinin Octapeptide Transport

2008 • 64 citations

In Vitro and Pharmacophore-Based Discovery of Novel hPEPT1 Inhibitors

2005 • 63 citations

Mechanistic Modeling of Hepatic Transport from Cells to Whole Body: Application to Napsagatran and Fexofenadine

2009 • 61 citations

Ins and outs of the ABCG2 multidrug transporter: An update on in vitro functional assays

2008 • 60 citations

Stereoselective inhibition of pindolol renal clearance by cimetidine in humans

1992 • 58 citations

Biochemical and Molecular Pharmacological Aspects of Transporters as Determinants of Drug Disposition

2005 • 57 citations

Val133 and Cys137 in Transmembrane Segment 2 Are Close to Arg935 and Gly939 in Transmembrane Segment 11 of Human P-glycoprotein

2004 • 56 citations

Effect of cimetidine and probenecid on pilsicainide renal clearance in humans

2000 • 53 citations

Future directions for drug transporter modelling

2007 • 53 citations

Severe arrhythmia as a result of the interaction of cetirizine and pilsicainide in a patient with renal insufficiency: First case presentation showing competition for excretion via renal multidrug resistance protein 1 and organic cation transporter 2

2006 • 51 citations

In vivo imaging of hepatobiliary transport function mediated by multidrug resistance associated protein and P-glycoprotein

2004 • 51 citations

Blood–brain barrier transport of pramipexole, a dopamine D2 agonist

2007 • 48 citations

Action of EGF and PGE2on basolateral organic anion uptake in rabbit proximal renal tubules and hOAT1 expressed in human kidney epithelial cells

2004 • 46 citations

Uptake and Efflux Transporters for Conjugates in Human Hepatocytes

2005 • 45 citations

High‐Speed Screening of Human ATP‐Binding Cassette Transporter Function and Genetic Polymorphisms: New Strategies in Pharmacogenomics

2005 • 45 citations

Knocking Down Breast Cancer Resistance Protein (Bcrp) by Adenoviral Vector-Mediated RNA Interference (RNAi) in Sandwich-Cultured Rat Hepatocytes: A Novel Tool To Assess the Contribution of Bcrp to Drug Biliary Excretion

2008 • 44 citations

A novel method for the determination of biliary clearance in humans

2004 • 43 citations

Pharmacogenetics of Membrane Transporters: A Review of Current Approaches

2014 • 41 citations

Optimising drug development: strategies to assess drug metabolism/transporter interaction potential — towards a consensus

2001 • 40 citations

Mini Review on Molecular Modeling of P-Glycoprotein (Pgp)

2007 • 38 citations

Noninvasive assessment of hepatobiliary and renal elimination of cysteinyl leukotrienes by positron emission tomography

1995 • 37 citations

siRNA—Getting the message out

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Dual Hereditary Jaundice: Simultaneous Occurrence of Mutations Causing Gilbert’s and Dubin-Johnson Syndrome

2005 • 35 citations

Studies of Human MDR1-MDR2 Chimeras Demonstrate the Functional Exchangeability of a Major Transmembrane Segment of the Multidrug Transporter and Phosphatidylcholine Flippase

1999 • 33 citations

Analysis of Catalytic Carboxylate Mutants E552Q and E1197Q Suggests Asymmetric ATP Hydrolysis by the Two Nucleotide-Binding Domains of P-Glycoprotein

2003 • 33 citations

Relationship of Hepatic Functional Imaging to Irinotecan Pharmacokinetics and Genetic Parameters of Drug Elimination

2006 • 32 citations

Tariquidar, a Selective P-glycoprotein Inhibitor, Does Not Potentiate Loperamide’s Opioid Brain Effects in Humans despite Full Inhibition of Lymphocyte P-glycoprotein

2008 • 31 citations

Difference between pharmacokinetics of mycophenolic acid (MPA) in rats and that in humans is caused by different affinities of MRP2 to a glucuronized form.

2007 • 28 citations

Silencing the Breast Cancer Resistance Protein Expression and Function in Caco-2 Cells Using Lentiviral Vector-Based Short Hairpin RNA

2009 • 24 citations

Quinidine-digoxin interaction: are the pharmacokinetics of both drugs altered?

1985 • 23 citations

Data-Based Mathematical Modeling of Vectorial Transport across Double-Transfected Polarized Cells

2007 • 22 citations

Pharmacogenetics of Membrane Transporters

2008 • 22 citations

Caki-1 Cells Represent an in vitro Model System for Studying the Human Proximal Tubule Epithelium

2007 • 22 citations

Can celecoxib affect P-glycoprotein-mediated drug efflux? A microPET study

2008 • 19 citations

Low-affinity uptake of the fluorescent organic cation 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide (4-Di-1-ASP) in BeWo cells

2006 • 18 citations

99mTc-HIDA Cholescintigraphy in Children with Dubin-Johnson Syndrome

1983 • 13 citations

Caki-1 Cells as a Model System for the Interaction of Renally Secreted Drugs with OCT3

2008 • 13 citations

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Membrane transporters in drug development (2010) – Nature Reviews Drug Discovery | Metascience Observatory Explorer