Protein abundance of clinically relevant multidrug transporters along the entire length of the human intestine.

No abstract is available for this paper.

• Publication year

  2014

• Venue

  Molecular Pharmaceutics

• Publication date

  2014-09-11

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1021/mp500330yPMID 25158075
• 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.

• The Roles of MRP2, MRP3, OATP1B1, and OATP1B3 in Conjugated Hyperbilirubinemia

  2014cited by this paper
• Characterization of the Intestinal and Hepatic Uptake/Efflux Transport of the Magnetic Resonance Imaging Contrast Agent Gadolinium-Ethoxylbenzyl-Diethylenetriamine-Pentaacetic Acid

  2014cited by this paper
• Green Tea Ingestion Greatly Reduces Plasma Concentrations of Nadolol in Healthy Subjects

  2014cited by this paper
• Drug transport via the intestinal peptide transporter PepT1.

  2013cited by this paper
• Absolute abundance and function of intestinal drug transporters: a prerequisite for fully mechanistic in vitro-in vivo extrapolation of oral drug absorption.

  2013cited by this paper
• Emerging Transporters of Clinical Importance: An Update From the International Transporter Consortium

  2013cited by this paper
• Intestinal drug transporters: an overview.

  2013cited by this paper
• LC-MS/MS-based quantification of clinically relevant intestinal uptake and efflux transporter proteins.

  2013cited by this paper
• Transporters and Drug-Drug Interactions: Important Determinants of Drug Disposition and Effects

  2013cited by this paper
• Intestinal OATP1A2 inhibition as a potential mechanism for the effect of grapefruit juice on aliskiren pharmacokinetics in healthy subjects

  2012cited by this paper
• Oral drug delivery utilizing intestinal OATP transporters.

  2012cited by this paper
• Pharmaceutical excipients influence the function of human uptake transporting proteins.

  2012cited by this paper
• Pharmacokinetic Effects of Bariatric Surgery

  2012cited by this paper
• Oral Availability of Cefadroxil Depends on ABCC3 and ABCC4

  2012cited by this paper
• Construction, identification and application of HeLa cells stably transfected with human PEPT1 and PEPT2.

  2012cited by this paper
• Absolute immunoquantification of the expression of ABC transporters P-glycoprotein, breast cancer resistance protein and multidrug resistance-associated protein 2 in human liver and duodenum.

  2012cited by this paper
• Drug Interactions Between the Immunosuppressant Tacrolimus and the Cholesterol Absorption Inhibitor Ezetimibe in Healthy Volunteers

  2011cited by this paper
• Role of the intestinal bile acid transporters in bile acid and drug disposition.

  2011cited by this paper
• Vectorial transport of fexofenadine across Caco-2 cells: involvement of apical uptake and basolateral efflux transporters.

  2011cited by this paper
• Quantitative targeted absolute proteomics of human blood–brain barrier transporters and receptors

  2011cited by this paper
• Down-Regulation of ATP-Binding Cassette C2 Protein Expression in HepG2 Cells after Rifampicin Treatment Is Mediated by MicroRNA-379

  2011cited by this paper
• Genetic and Epigenetic Regulation of the Organic Cation Transporter 3, SLC22A3

  2011cited by this paper
• Molecular mechanisms of drug transporter regulation.

  2011cited by this paper
• Membrane transporters in drug development

  2010cited by this paper
• Significant Increase in Systemic Exposure of Atorvastatin After Biliopancreatic Diversion With Duodenal Switch

  2010cited by this paper
• Genetic variants in multidrug and toxic compound extrusion-1, hMATE1, alter transport function

  2009cited by this paper
• Changes in mRNA Expression Levels of Solute Carrier Transporters in Inflammatory Bowel Disease Patients

  2009cited by this paper
• Bioavailability of amoxicillin and clavulanic acid from extended release tablets depends on intragastric tablet deposition and gastric emptying.

  2008cited by this paper
• New Era in Drug Interaction Evaluation: US Food and Drug Administration Update on CYP Enzymes, Transporters, and the Guidance Process

  2008cited by this paper
• Gene and protein expression of P-glycoprotein, MRP1, MRP2, and CYP3A4 in the small and large human intestine.

  2007cited by this paper
• Expression of Thirty-six Drug Transporter Genes in Human Intestine, Liver, Kidney, and Organotypic Cell Lines

  2007cited by this paper
• The role of the intestine in drug metabolism and pharmacokinetics: an industry perspective.

  2007cited by this paper
• Regional Distribution of Solute Carrier mRNA Expression Along the Human Intestinal Tract

  2007cited by this paper
• Efflux transporters in ulcerative colitis: Decreased expression of BCRP (ABCG2) and Pgp (ABCB1)

  2007cited by this paper
• Intestinal Drug Transporter Expression and the Impact of Grapefruit Juice in Humans

  2007cited by this paper
• A "Silent" Polymorphism in the MDR1 Gene Changes Substrate Specificity

  2007cited by this paper
• Variability in mRNA expression of ABC- and SLC-transporters in human intestinal cells: comparison between human segments and Caco-2 cells.

  2006cited by this paper
• Regional levels of drug transporters along the human intestinal tract: co-expression of ABC and SLC transporters and comparison with Caco-2 cells.

  2006cited by this paper
• Effects of controlled-release on the pharmacokinetics and absorption characteristics of a compound undergoing intestinal efflux in humans.

  2006cited by this paper
• Intestinal expression of P‐glycoprotein (ABCB1), multidrug resistance associated protein 2 (ABCC2), and uridine diphosphate–glucuronosyltransferase 1A1 predicts the disposition and modulates the effects of the cholesterol absorption inhibitor ezetimibe in humans

  2006cited by this paper
• Grapefruit Juice Ingestion Significantly Reduces Talinolol Bioavailability

  2005cited by this paper
• The Talinolol Double-Peak Phenomenon Is Likely Caused by Presystemic Processing After Uptake from Gut Lumen

  2005cited by this paper
• Intestinal fluid volumes and transit of dosage forms as assessed by magnetic resonance imaging

  2005cited by this paper
• MAPPING OF MULTIDRUG RESISTANCE GENE 1 AND MULTIDRUG RESISTANCE-ASSOCIATED PROTEIN ISOFORM 1 TO 5 mRNA EXPRESSION ALONG THE HUMAN INTESTINAL TRACT

  2005cited by this paper
• CYP2D6 genotype and induction of intestinal drug transporters by rifampin predict presystemic clearance of carvedilol in healthy subjects

  2004cited by this paper
• P-Glycoprotein Increases from Proximal to Distal Regions of Human Small Intestine

  2003cited by this paper
• Fruit juices inhibit organic anion transporting polypeptide–mediated drug uptake to decrease the oral availability of fexofenadine

  2002cited by this paper
• Polymorphisms in OATP-C

  2001cited by this paper
• P-glycoprotein inhibitor erythromycin increases oral bioavailability of talinolol in humans.

  2000cited by this paper
• Induction of P‐glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: A new type of drug/drug interaction

  2000cited by this paper
• Relevance of p‐glycoprotein for the enteral absorption of cyclosporin A: in vitro‐in vivo correlation

  1996cited by this paper
• Direct demonstration of small intestinal secretion and site‐dependent absorption of the β‐blocker talinolol in humans

  1996cited by this paper
• Differential absorption of amoxicillin from the human small and large intestine

  1994cited by this paper
• Measurement of gastrointestinal pH profiles in normal ambulant human subjects.

  1988cited by this paper
• Bioavailability study of a new amoxicillin tablet designed for several modes of oral administration.

  1987cited by this paper
• Supporting Online Material Materials and Methods Som Text Figs. S1 to S8 Table S1 Movies S1 to S3 a " Silent " Polymorphism in the Mdr1 Gene Changes Substrate Specificity Corrected 30 November 2007; See Last Page

  year unknowncited by this paper

• Characterization of EpiIntestinal Duodenum Microtissue as an In Vitro Model for Studying Intestinal Drug Permeability, Transport, and Metabolism.

  2026cites this paper
• Biological pathways of per- and polyfluoroalkyl substances (PFAS): A critical review of cellular and molecular toxicity mechanisms.

  2026cites this paper
• The Role of Short-Chain Fatty Acids Produced by Oral Bacteria in Modulating Oral Immunity.

  2026cites this paper
• Quantitative Analysis of the Effect of Gastrointestinal Water Dynamics on Oral Drug Absorption using a Physiologically Based Integrated Liquid and Intestinal Absorption Drug (ILIAD) Pharmacokinetic Model.

  2026cites this paper
• SLC52A1 Is a Neofunctionalized Primate Urate Transporter Enabling Intestinal Urate Secretion.

  2026cites this paper
• Regional absorption of talinolol mediated by intestinal transporters: insights from PBPK modeling analysis.

  2026cites this paper
• Rosuvastatin PBPK Modeling: Incorporating Liver Concentrations and Effects of Ethnicity, Genetic Polymorphisms, Lactone Formation, DDI and Pregnancy

  2025cites this paper
• Characterization of intestinal transporters in human ileal spheroid-derived differentiated cells for the prediction of intestinal drug absorption.

  2025cites this paper
• Protein abundance of drug transporters and drug-metabolizing enzymes in paired healthy and tumor tissue from colorectal cancer patients.

  2025cites this paper
• Characterization of small molecule drug clearance mechanisms using in vitro and in vivo approaches in drug discovery and development

  2025cites this paper
• Harnessing the apical sodium-dependent bile acid transporter for enhanced oral delivery of peptide drugs: mechanisms, strategies, and therapeutic potential

  2025cites this paper
• In Vitro Characterization of SLCO2B1 Genetic Variants.

  2025cites this paper
• Significance of gut breast cancer resistance protein versus organic anion transporting polypeptide 2B1 inhibition on rosuvastatin clinical drug-drug interactions.

  2025cites this paper
• A gut response: Application of human enteroid monolayers to probe the mechanism of the goldenseal-mediated inhibition of metformin intestinal absorption.

  2025cites this paper
• Oral Peptide Delivery Reimagined: Molecular Barriers, Formulation Strategies, and the Rise of Computational Design

  2025cites this paper
• Possible interactions between selected food processing and medications

  2024cites this paper
• Expression of intestinal drug transporter proteins and metabolic enzymes in neonatal and pediatric patients.

  2024cites this paper
• Organic anion transporting polypeptides: Pharmacology, toxicology, structure, and transport mechanisms.

  2024cites this paper
• Distribution Characteristics and Impacting Factors of Drug CYP Enzymes and Transporters in the Gastrointestinal Tract of Chinese Healthy Subjects

  2024cites this paper
• Mechanisms of intestinal pharmacokinetic natural product-drug interactions

  2024cites this paper
• Intestinal absorption mechanism and nutritional synergy promotion strategy of dietary flavonoids: transintestinal epithelial pathway mediated by intestinal transport proteins

  2024cites this paper
• Age-Specific ADME Gene Expression in Infant Intestinal Enteroids

  2024cites this paper
• A Continuous Intestinal Absorption Model to Predict Drug Enterohepatic Recirculation in Healthy Humans: Nalbuphine as a Model Substrate.

  2024cites this paper
• Differential Tissue Abundance of Membrane-Bound Drug Metabolizing Enzymes and Transporter Proteins by Global Proteomics

  2024cites this paper
• FOCUS on NOD2: Advancing IBD Drug Discovery with a User-Informed Machine Learning Framework.

  2024cites this paper
• Intestinal transporters and oral absorption enhancing strategies based on these transporters

  2024cites this paper
• Membrane transporters in drug development and as determinants of precision medicine

  2024influential citation
• Pharmacokinetics-based identification of antiviral compounds of Rheum palmatum rhizomes and roots (Dahuang)

  2023cites this paper
• Quantification of drug metabolising enzymes and transporter proteins in the paediatric duodenum via LC-MS/MS proteomics using a QconCAT technique.

  2023cites this paper
• The impact of advanced age on gastrointestinal characteristics that are relevant to oral drug absorption: An AGePOP review.

  2023cites this paper
• Recent Advances in the Gastrointestinal Complex in Vitro Model for ADME Studies

  2023cites this paper
• Effects of schisandra lignans on the absorption of protopanaxadiol-type ginsenosides mediated by P-glycoprotein and protopanaxatriol-type ginsenosides mediated by CYP3A4.

  2023cites this paper
• Insights into Intestinal P-glycoprotein Function using Talinolol: A PBPK Modeling Approach

  2023cites this paper
• Regional Transcriptomics and Proteomics of Pharmacokinetics-Related Genes in Human Intestine.

  2023cites this paper
• Surface engineering of chitosan nanosystems and the impact of functionalized groups on the permeability of model drug across intestinal tissue.

  2023cites this paper
• Interplay of Breast Cancer Resistance Protein (Bcrp/Abcg2), Sex, and Fed State in Oral Pharmacokinetic Variability of Furosemide in Rats

  2023cites this paper
• Quantitative Characterization of Clinically Relevant Drug-Metabolizing Enzymes and Transporters in Rat Liver and Intestinal Segments for Applications in PBPK Modeling.

  2023cites this paper
• Intestinal organoids as an in vitro platform to characterize disposition, metabolism, and safety profile of small molecules.

  2023cites this paper
• Low dose daily folic acid (400 μg) supplementation does not affect regulation of folate transporters found present throughout the terminal ileum and colon of humans: a randomized clinical trial.

  2023cites this paper
• Analysis of Complex Absorption After Multiple Dosing: Application to the Interaction Between the P-glycoprotein Substrate Talinolol and Rifampicin

  2022cites this paper
• The impact of inflammation on the expression of drug transporters and metabolic enzymes in colonic tissue from ulcerative colitis patients.

  2022cites this paper
• Usefulness of Human Jejunal Spheroid–Derived Differentiated Intestinal Epithelial Cells for the Prediction of Intestinal Drug Absorption in Humans

  2022cites this paper
• Inhibitory Effects of Cranberry Juice and Its Components on Intestinal OATP1A2 and OATP2B1: Identification of Avicularin as a Novel Inhibitor.

  2022cites this paper
• Food effects on gastrointestinal physiology and drug absorption.

  2022cites this paper
• Synergistic Hypolipidemic Effects and Mechanisms of Phytochemicals: A Review

  2022cites this paper
• Drug Disposition in the Lower Gastrointestinal Tract: Targeting and Monitoring

  2021cites this paper
• Adaptations in gastrointestinal physiology after sleeve gastrectomy and Roux-en-Y gastric bypass.

  2021cites this paper
• Constituents of Passiflora incarnata, but Not of Valeriana officinalis, Interact with the Organic Anion Transporting Polypeptides (OATP)2B1 and OATP1A2

  2021cites this paper
• Impact of gastrointestinal tract variability on oral drug absorption and pharmacokinetics: an UNGAP review.

  2021cites this paper
• Organic Cation Transporter 1 an Intestinal Uptake Transporter: Fact or Fiction?

  2021cites this paper
• [Pharmacokinetic interactions of fruit juices and herbal preparations].

  2021cites this paper
• Ad-Apoptin-hTERTp-E1a Regulates Autophagy Through the AMPK-mTOR-eIF4F Signaling Axis to Reduce Drug Resistance of MCF-7/ADR Cells

  2021cites this paper
• Role of Membrane Transporters in Drug Disposition

  2021cites this paper
• Gutsy science: In vitro systems of the human intestine to model oral drug disposition.

  2021cites this paper
• Structural snapshots of human PepT1 and PepT2 reveal mechanistic insights into substrate and drug transport across epithelial membranes

  2021cites this paper
• Role of uptake transporters OAT4, OATP2A1, and OATP1A2 in human placental bio-disposition of pravastatin.

  2021cites this paper
• A Non-Nutritive Feeding Intervention Alters the Expression of Efflux Transporters in the Gastrointestinal Tract

  2021cites this paper
• Cynomolgus Monkey as an Emerging Animal Model to Study Drug Transporters: In Vitro, In Vivo, In Vitro-to-In Vivo Translation

  2021cites this paper
• Ontogeny of Small Intestinal Drug Transporters and Metabolizing Enzymes Based on Targeted Quantitative Proteomics

  2021cites this paper
• Pharmacogenomics of celiprolol – evidence for a role of P‐glycoprotein and organic anion transporting polypeptide 1A2 in celiprolol pharmacokinetics

  2021cites this paper
• Pharmacokinetic Modeling of Morphine’s Effect on Plasma Concentrations of Ticagrelor and Its Metabolite in Healthy Volunteers

  2021cites this paper
• Transporter-mediated drug–drug interactions: advancement in models, analytical tools, and regulatory perspective

  2021cites this paper
• Quantification of P-Glycoprotein in the Gastrointestinal Tract of Humans and Rodents: Methodology, Gut Region, Sex, and Species Matter

  2021cites this paper
• Challenges of peptide and protein drug delivery by oral route: Current strategies to improve the bioavailability

  2021cites this paper
• Physiologically Based Pharmacokinetic Modeling of Cefadroxil in Mouse, Rat, and Human to Predict Concentration–Time Profile at Infected Tissue

  2021cites this paper
• A Whole-Body Physiologically Based Pharmacokinetic Model Characterizing Interplay of OCTs and MATEs in Intestine, Liver and Kidney to Predict Drug-Drug Interactions of Metformin with Perpetrators

  2021cites this paper
• Prognostic Significance of Autophagy-Relevant Gene Markers in Colorectal Cancer

  2021cites this paper
• Quantitative analysis of the effect of controlled-release formulation on nonlinear gastrointestinal absorption of P-glycoprotein substrate talinolol using physiologically based pharmacokinetic absorption model

  2020cites this paper
• Interactions of Oral Molecular Excipients with Breast Cancer Resistance Protein, BCRP.

  2020cites this paper
• Enteral Medication for the Tube-Fed Patient: Making This Route Safe and Effective.

  2020cites this paper
• Role of transporters in drug disposition and drug-drug interactions

  2020cites this paper
• Organic Cation Transporters in Health and Disease

  2020cites this paper
• Quantitative Proteomics of Clinically Relevant Drug-Metabolizing Enzymes and Drug Transporters and Their Intercorrelations in the Human Small Intestine

  2020influential citation
• Citrus Fruit-Derived Flavanone Glycoside Narirutin is a Novel Potent Inhibitor of Organic Anion-Transporting Polypeptides.

  2020cites this paper
• Mass spectrometry‐based abundance atlas of ABC transporters in human liver, gut, kidney, brain and skin

  2020cites this paper
• Equine Drug Transporters: A Mini-Review and Veterinary Perspective

  2020cites this paper
• Quantifying drug metabolizing enzymes and transporters by LC-MS/MS proteomics

  2020cites this paper
• Physiologically Based Pharmacokinetic/Pharmacodynamic Modeling to Support Waivers of In Vivo Clinical Studies: Current Status, Challenges, and Opportunities.

  2020cites this paper
• In vivo modulation of cervicovaginal drug transporters and tissue distribution by film-released tenofovir and darunavir for topical prevention of HIV-1.

  2020cites this paper
• Food additives as inhibitors of intestinal drug transporter OATP2B1.

  2020cites this paper
• Current Understanding of the Intestinal Absorption of Nucleobases and Analogs.

  2020cites this paper
• Using Ex Vivo Porcine Jejunum to Identify Membrane Transporter Substrates: A Screening Tool for Early—Stage Drug Development

  2020cites this paper
• Boosting drug bioavailability in men but not women through the action of 1 an excipient 2 3

  2020cites this paper
• A Pharmacokinetic Bridging Study to Compare Systemic Exposure to Budesonide between Budesonide Oral Suspension and ENTOCORT EC in Healthy Individuals

  2020cites this paper
• Intestinal drug transporters in pathological states: an overview

  2020cites this paper
• Extrahepatic Drug Transporters in Liver Failure: Focus on Kidney and Gastrointestinal Tract

  2020influential citation
• Role of membrane-embedded drug efflux ABC transporters in the cancer chemotherapy

  2020cites this paper
• Inter‐individual and inter‐regional variations in enteric drug metabolizing enzyme activities: Results with cryopreserved human intestinal mucosal epithelia (CHIM) from the small intestines of 14 donors

  2020cites this paper
• Boosting drug bioavailability in men but not women through the action of an excipient.

  2020cites this paper
• Metformin Transport in Native MDCK-Wt and MDCK-II Monolayers Unveils Functional Inter-Strains Differences Influencing Drug Permeability

  2020influential citation
• A Physiologically-based Drug Absorption Modeling for Orally Disintegrating Tablets.

  2020cites this paper
• Physiologically-Based Pharmacokinetic Predictions of the Effect of Curcumin on Metabolism of Imatinib and Bosutinib: In Vitro and In Vivo Disconnect

  2020cites this paper
• An intact C-terminal end of albumin is required for its long half-life in humans

  2020cites this paper
• Apical sodium-dependent bile acid transporter, drug target for bile acid related diseases and delivery target for prodrugs: Current and future challenges.

  2020cites this paper
• Effect of Food and an Animal’s Sex on P-Glycoprotein Expression and Luminal Fluids in the Gastrointestinal Tract of Wistar Rats

  2020cites this paper
• Relevance of Transporters in Clinical Studies

  2020cites this paper
• Pharmacokinetics of Gemcitabine and its Amino Acid Ester Prodrug following Intravenous and Oral Administrations in Mice.

  2020cites this paper
• Mass Spectrometry of Human Transporters.

  2020cites this paper
• Impact of gastrointestinal physiology on drug absorption in special populations - An UNGAP review.

  2020cites this paper
• Type 2 diabetes mellitus decreases systemic exposure of clopidogrel active metabolite through upregulation of P-glycoprotein in rats.

  2020cites this paper