ArticlePharmaceutical research2009
Identification of novel specific and general inhibitors of the three major human ATP-binding cassette transporters P-gp, BCRP and MRP2 among registered drugs.
Article in Pharmaceutical research, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 115 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
115 citing papers in PubMed, 312 citations in OpenAlex.
- Urinary coproporphyrin I/(I + III) ratio as a surrogate for MRP2 or other transporter activities involved in methotrexate clearance.British journal of clinical pharmacology · 2014Trial
- In Silico Regression Modeling and Improved Interpretability To Predict the Transport Inhibitory Activity of Breast Cancer Resistance Protein.ACS omega · 2026Article
- Article
- Dicloxacillin and Flucloxacillin Inhibit Hepatic Uptake Transporters-In Vitro Investigations and Physiologically Based Pharmacokinetic Modeling.Clinical and translational science · 2026Article
- Characterization of EpiIntestinal Duodenum Microtissue as an In Vitro Model for Studying Intestinal Drug Permeability, Transport, and Metabolism.Pharmaceutical research · 2026Article
- Elacridar Reverses P-gp-Mediated Drug Resistance in Ovarian Cancer Cells in 2D and 3D Culture Models.International journal of molecular sciences · 2025Article
- Dicloxacillin and flucloxacillin inhibit hepatic uptake transporters -in vitro investigations and physiologically based pharmacokinetic modelling.bioRxiv : the preprint server for biology · 2025Article
- Discovery of Novel Benzamide-Based Sigma-1 Receptor Agonists with Enhanced Selectivity and Safety.Molecules (Basel, Switzerland) · 2025Article
- Food Additives Inhibit Intestinal Drug Transporters but Have Limited Effect on In Vitro Drug Permeability.Molecular pharmaceutics · 2025Article
- Elacridar Inhibits BCRP Protein Activity in 2D and 3D Cell Culture Models of Ovarian Cancer and Re-Sensitizes Cells to Cytotoxic Drugs.International journal of molecular sciences · 2025Article
- Reliability of in vitro data for the mechanistic prediction of brain extracellular fluid pharmacokinetics of P-glycoprotein substrates in vivo; are we scaling correctly?Journal of pharmacokinetics and pharmacodynamics · 2025Article
- The Role of Elacridar, a P-gp Inhibitor, in the Re-Sensitization of PAC-Resistant Ovarian Cancer Cell Lines to Cytotoxic Drugs in 2D and 3D Cell Culture Models.International journal of molecular sciences · 2025Article
- Towards streamlined product information: reporting of transporter-mediated drug interactions.European journal of clinical pharmacology · 2025Article
- Knockout Transporter Cell Lines to Assess Substrate Potential Towards Efflux Transporters.The AAPS journal · 2024Article
- The role of membrane transporters in the absorption of atrazine following nasal exposure.Inhalation toxicology · 2024Article
- Effects of Aqueous Boundary Layers and Paracellular Transport on the Efflux Ratio as a Measure of Active Transport Across Cell Layers.Pharmaceutics · 2024Article
- Evaluation of Encequidar as An Intestinal P-gp and BCRP Specific Inhibitor to Assess the Role of Intestinal P-gp and BCRP in Drug-Drug Interactions.Pharmaceutical research · 2023Article
- Transporter Inhibition Profile for the Antivirals Tilorone, Quinacrine and Pyronaridine.ACS omega · 2023Article
- ABCB1 expression is increased in human first trimester placenta from pregnant women classified as overweight or obese.Scientific reports · 2023Article
- P-glycoprotein (ABCB1) - weak dipolar interactions provide the key to understanding allocrite recognition, binding, and transport.Cancer drug resistance (Alhambra, Calif.) · 2023Review
55 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo study the inhibition patterns of the three major human ABC transporters P-gp (ABCB1), BCRP (ABCG2) and MRP2 (ABCC2), using a dataset of 122 structurally diverse drugs.
methodsInhibition was investigated in cellular and vesicular systems over-expressing single transporters. Computational models discriminating either single or general inhibitors from non-inhibitors were developed using multivariate statistics.
resultsSpecific (n = 23) and overlapping (n = 19) inhibitors of the three ABC transporters were identified. GF120918 and Ko143 were verified to specifically inhibit P-gp/BCRP and BCRP in defined concentration intervals, whereas the MRP inhibitor MK571 was revealed to inhibit all three transporters within one log unit of concentration. Virtual docking experiments showed that MK571 binds to the ATP catalytic site, which could contribute to its multi-specific inhibition profile. A computational model predicting general ABC inhibition correctly classified 80% of both ABC transporter inhibitors and non-inhibitors in an external test set.
conclusionsThe inhibitor specificities of P-gp, BCRP and MRP2 were shown to be highly overlapping. General ABC inhibitors were more lipophilic and aromatic than specific inhibitors and non-inhibitors. The identified specific inhibitors can be used to delineate transport processes in complex experimental systems, whereas the multi-specific inhibitors are useful in primary ABC transporter screening in drug discovery settings.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.