ReviewPharmaceutical research2005
Apical/basolateral surface expression of drug transporters and its role in vectorial drug transport.
Review in Pharmaceutical research, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.
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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
45 citing papers in PubMed, 172 citations in OpenAlex.
- Assessment of a candidate marker constituent predictive of a dietary substance-drug interaction: case study with grapefruit juice and CYP3A4 drug substrates.The Journal of pharmacology and experimental therapeutics · 2014Trial
- SLCO1B1 521T-->C functional genetic polymorphism and lipid-lowering efficacy of multiple-dose pravastatin in Chinese coronary heart disease patients.British journal of clinical pharmacology · 2007Trial
- Optimization of Methods for the Quantitative Analysis of Global Cell Surface Proteome and Cell Surface Polarization.International journal of molecular sciences · 2025Article
- Standard Protocols for Characterising Primary and In Vitro-Generated Human Hepatocytes.Journal of cellular and molecular medicine · 2025Review
- The pH-dependence of efflux ratios determined with bidirectional transport assays across cellular monolayers.International journal of pharmaceutics: X · 2024Article
- Assessment of clinically actionable pharmacogenetic markers to stratify anti-seizure medications.The pharmacogenomics journal · 2023Article
- Article
- Optimization of extracellular matrix for primary human hepatocyte cultures using mixed collagen-Matrigel matrices.EXCLI journal · 2023Article
- Oligomeric proanthocyanidins (OPCs) from grape seed extract suppress the activity of ABC transporters in overcoming chemoresistance in colorectal cancer cells.Carcinogenesis · 2019Article
- Epithelial Cells and Fibroblasts from the Human Female Reproductive Tract Accumulate and Release TFV and TAF to Sustain Inhibition of HIV Infection of CD4+ T cells.Scientific reports · 2019Article
- Effects of emodin on ABC transporter gene expression in grass carp (Ctenopharyngodon idellus) exposed to diazinon.PloS one · 2019Article
- Pharmacokinetic Drug Interactions with Panax ginseng.European journal of drug metabolism and pharmacokinetics · 2017Review
- Quantitative Evaluation of Drug Resistance Profile of Cells Expressing Wild-Type or Genetic Polymorphic Variants of the Human ABC Transporter ABCC4.International journal of molecular sciences · 2017Article
- Cellular Models and In Vitro Assays for the Screening of modulators of P-gp, MRP1 and BCRP.Molecules (Basel, Switzerland) · 2017Review
- Noninvasive Assessment of Elimination and Retention using CT-FMT and Kinetic Whole-body Modeling.Theranostics · 2017Article
- A Physiologically Based Pharmacokinetic Model for Ganciclovir and Its Prodrug Valganciclovir in Adults and Children.The AAPS journal · 2016Article
- Physiological and molecular biochemical mechanisms of bile formation.World journal of gastroenterology · 2013Review
- Which drug or drug delivery system can change clinical practice for brain tumor therapy?Neuro-oncology · 2013Review
- Cell-penetrating Peptide-mediated therapeutic molecule delivery into the central nervous system.Current neuropharmacology · 2013Article
- Influence of overexpression of efflux proteins on the function and gene expression of endogenous peptide transporters in MDR-transfected MDCKII cell lines.International journal of pharmaceutics · 2013Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
It is well known that transporter proteins play a key role in governing drug absorption, distribution, and elimination in the body, and, accordingly, they are now considered as causes of drug-drug interactions and interindividual differences in pharmacokinetic profiles. Polarized tissues directly involved in drug disposition (intestine, kidney, and liver) and restricted distribution to naive sanctuaries (blood-tissue barriers) asymmetrically express a variety of drug transporters on the apical and basolateral sides, resulting in vectorial drug transport. For example, the organic anion transporting polypeptide (OATP) family on the sinusoidal (basolateral) membrane and multidrug resistance-associated protein 2 (MRP2/ABCC2) on the apical bile canalicular membrane of hepatocytes take up and excrete organic anionic compounds from blood to bile. Such vectorial transcellular transport is fundamentally attributable to the asymmetrical distribution of transporter molecules in polarized cells. Besides the apical/basolateral sorting direction, distribution of the transporter protein between the membrane surface (active site) and the intracellular fraction (inactive site) is of practical importance for the quantitative evaluation of drug transport processes. The most characterized drug transporter associated with this issue is MRP2 on the hepatocyte canalicular (apical) membrane, and it is linked to a genetic disease. Dubin-Johnson syndrome is sometimes caused by impaired canalicular surface expression of MRP2 by a single amino acid substitution. Moreover, single nucleotide polymorphisms in OATP-C/SLC21A6 (SLCO1B1) also affect membrane surface expression, and actually lead to the altered pharmacokinetic profile of pravastatin in healthy subjects. In this review article, the asymmetrical transporter distribution and altered surface expression in polarized tissues are discussed.
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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.