ArticleNaunyn-Schmiedeberg's archives of pharmacology2009
A novel screening strategy to identify ABCB1 substrates and inhibitors.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers, 1 of them a synthesis that pooled it.
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
21 citing papers in PubMed, 1 synthesis or guideline pooled it, 69 citations in OpenAlex.
- Meta-Analysis of Permeability Literature Data Shows Possibilities and Limitations of Popular Methods.Molecular pharmaceutics · 2025Pooled it
- Elucidating the Complex Structural and Molecular Mechanisms Driving P-Glycoprotein-Mediated Transport of Cardiac Glycosides.International journal of molecular sciences · 2025Article
- Applicability of MDR1 Overexpressing Abcb1KO-MDCKII Cell Lines for Investigating In Vitro Species Differences and Brain Penetration Prediction.Pharmaceutics · 2024Article
- Differing temperature dependencies of functional homologs zebrafish Abcb4 and human ABCB1.Frontiers in pharmacology · 2024Article
- Differential Action of Silver Nanoparticles on ABCB1 (MDR1) and ABCC1 (MRP1) Activity in Mammalian Cell Lines.Materials (Basel, Switzerland) · 2021Article
- Disruption of small molecule transporter systems by Transporter-Interfering Chemicals (TICs).FEBS letters · 2020Review
- Environmental mechanisms of orofacial clefts.Birth defects research · 2020Review
- ABC transporters and the hallmarks of cancer: roles in cancer aggressiveness beyond multidrug resistance.Cancer biology & medicine · 2020Review
- Micelle-Forming Block Copolymers Tailored for Inhibition of P-gp-Mediated Multidrug Resistance: Structure to Activity Relationship.Pharmaceutics · 2019Article
- Insights Into the Molecular Mechanism of Triptan Transport by P-glycoprotein.Journal of pharmaceutical sciences · 2017Article
- Predicting apparent passive permeability of Caco-2 and MDCK cell-monolayers: A mechanistic model.PloS one · 2017Article
- Unravelling the complex drug-drug interactions of the cardiovascular drugs, verapamil and digoxin, with P-glycoprotein.Bioscience reports · 2016Article
- Membrane Assays to Characterize Interaction of Drugs with ABCB1.The Journal of membrane biology · 2015Article
- Cell-free microfluidic determination of P-glycoprotein interactions with substrates and inhibitors.Pharmaceutical research · 2014Article
- Challenges of using in vitro data for modeling P-glycoprotein efflux in the blood-brain barrier.Pharmaceutical research · 2014Review
- Use of different parameters and equations for calculation of IC₅₀ values in efflux assays: potential sources of variability in IC₅₀ determination.The AAPS journal · 2014Article
- Cost, effectiveness and environmental relevance of multidrug transporters in sea urchin embryos.The Journal of experimental biology · 2013Article
- Abcb4 acts as multixenobiotic transporter and active barrier against chemical uptake in zebrafish (Danio rerio) embryos.BMC biology · 2013Article
- Interactions between antidepressants and P-glycoprotein at the blood-brain barrier: clinical significance of in vitro and in vivo findings.British journal of pharmacology · 2012Review
- A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.Journal of medicinal chemistry · 2011Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We tested the hypothesis whether data on ABCB1 ATPase activity and passive permeability can be used in combination to identify ABCB1 substrates and inhibitors. We determined passive permeability using an artificial membrane permeability assay (HDM-PAMPA) and ABCB1 function, i.e., vanadate-sensitive ATPase activity for a training set (40 INN drugs) and a validation set (26 development compounds). In parallel experiments, we determined ABCB1 function, i.e., vectorial transport in a Caco-2 cell monolayer, and ABCB1 inhibition, i.e., calcein AM extrusion out of K562-MDR cells, to cross-validate the results with cellular assays. We found that compounds that did not modulate ABCB1-ATPase did also not affect calcein AM extrusion and were not actively transported by ABCB1 in Caco-2 cell monolayers. The results corroborated the effect of passive permeability as an important covariate of active transport: active transport in Caco-2 monolayer was only apparent for compounds showing low passive permeability (<5.0 cmx10(-6)/s) in the HDM-PAMPA assay whereas compounds with high passive permeability (>50 cmx10(-6)/s) were shown to inhibit calcein AM efflux with IC50 values close to their respective Km value obtained for ABCB1-ATPase. The use of HDM-PAMPA in combination with ABCB1-ATPase offers a simple, inexpensive experimental approach capable of identifying ABCB1 inhibitors as well as transported substrates.
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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.