ArticleTrends in pharmacological sciences2015
Fitting Transporter Activities to Cellular Drug Concentrations and Fluxes: Why the Bumblebee Can Fly.
Article in Trends in pharmacological sciences, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Multi-species assessment of propranolol pharmacokinetics via minimal and whole-body PBPK modeling.Frontiers in pharmacology · 2026Article
- The Transporter-Mediated Cellular Uptake and Efflux of Pharmaceutical Drugs and Biotechnology Products: How and Why Phospholipid Bilayer Transport Is Negligible in Real Biomembranes.Molecules (Basel, Switzerland) · 2021Review
- Generation of a Small Library of Natural Products Designed to Cover Chemical Space Inexpensively.Pharmaceutical frontiers · 2019Article
- Energetic evolution of cellular Transportomes.BMC genomics · 2018Article
- Metabolic regulation is sufficient for global and robust coordination of glucose uptake, catabolism, energy production and growth in Escherichia coli.PLoS computational biology · 2017Article
- Analysis of drug-endogenous human metabolite similarities in terms of their maximum common substructures.Journal of cheminformatics · 2017Article
- Enhancing Drug Efficacy and Therapeutic Index through Cheminformatics-Based Selection of Small Molecule Binary Weapons That Improve Transporter-Mediated Targeting: A Cytotoxicity System Based on Gemcitabine.Frontiers in pharmacology · 2017Article
- Implications of endogenous roles of transporters for drug discovery: hitchhiking and metabolite-likeness.Nature reviews. Drug discovery · 2016Article
- The metabolome 18 years on: a concept comes of age.Metabolomics : Official journal of the Metabolomic Society · 2016Review
- MetMaxStruct: A Tversky-Similarity-Based Strategy for Analysing the (Sub)Structural Similarities of Drugs and Endogenous Metabolites.Frontiers in pharmacology · 2016Article
- Individuality, phenotypic differentiation, dormancy and 'persistence' in culturable bacterial systems: commonalities shared by environmental, laboratory, and clinical microbiology.F1000Research · 2015Review
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Abstract
A recent paper in this journal argued that reported expression levels, kcat and Km for drug transporters could be used to estimate the likelihood that drug fluxes through Caco-2 cells could be accounted for solely by protein transporters. It was in fact concluded that if five such transporters contributed 'randomly' they could account for the flux of the most permeable drug tested (verapamil) 35% of the time. However, the values of permeability cited for verapamil were unusually high; this and other drugs have much lower permeabilities. Even for the claimed permeabilities, we found that a single 'random' transporter could account for the flux 42% of the time, and that two transporters can achieve 10·10(-6)cm·s(-1) 90% of the time. Parameter optimisation methods show that even a single transporter can account for Caco-2 drug uptake of the most permeable drug. Overall, the proposal that 'phospholipid bilayer diffusion (of drugs) is negligible' is not disproved by the calculations of 'likely' transporter-based fluxes.
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