ArticleBiochemical pharmacology2018
Ligand-dependent modulation of hOCT1 transport reveals discrete ligand binding sites within the substrate translocation channel.
Article in Biochemical pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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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.
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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
17 citing papers in PubMed, 32 citations in OpenAlex.
- Evaluating the Utility and Constraints of the Competitive Counter Flow (CCF) Assay in OATP1B1 Substrate Profiling.The AAPS journal · 2026Article
- Effects of Chronic Elevation in Plasma Membrane Cholesterol on the Function of Human NaLivers · 2025Article
- Substrate Specificity of the Organic Cation Transporters MATE1 and MATE2K and Functional Overlap with OCT1 and OCT2.Journal of medicinal chemistry · 2025Article
- The Competitive Counterflow Assay for Identifying Drugs Transported by Solute Carriers: Principle, Applications, Challenges/Limits, and Perspectives.European journal of drug metabolism and pharmacokinetics · 2024Review
- Interaction and Transport of Benzalkonium Chlorides by the Organic Cation and Multidrug and Toxin Extrusion Transporters.Drug metabolism and disposition: the biological fate of chemicals · 2024Article
- Region-independent active CNS net uptake of marketed HFrontiers in cellular neuroscience · 2024Article
- Characterization of ligand-induced thermal stability of the human organic cation transporter 2 (OCT2).Frontiers in pharmacology · 2023Article
- Atypical Substrates of the Organic Cation Transporter 1.Biomolecules · 2022Article
- Amino acids in transmembrane helix 1 confer major functional differences between human and mouse orthologs of the polyspecific membrane transporter OCT1.The Journal of biological chemistry · 2022Article
- Using a competitive counterflow assay to identify novel cationic substrates of OATP1B1 and OATP1B3.Frontiers in physiology · 2022Article
- Untangling Absorption Mechanisms and Variability in Bioequivalence Studies Using Population Analysis.Pharmaceutical research · 2021Article
- Drug-Drug Interactions at Organic Cation Transporter 1.Frontiers in pharmacology · 2021Review
- Transport of Drugs and Endogenous Compounds Mediated by Human OCT1: Studies in Single- and Double-Transfected Cell Models.Frontiers in pharmacology · 2021Review
- OCT1 Polyspecificity-Friend or Foe?Frontiers in pharmacology · 2021Article
- Kinetic basis of metformin-MPP interactions with organic cation transporter OCT2.American journal of physiology. Renal physiology · 2019Article
- Current Advances in Studying Clinically Relevant Transporters of the Solute Carrier (SLC) Family by Connecting Computational Modeling and Data Science.Computational and structural biotechnology journal · 2019Review
- A clinically relevant polymorphism in the NaThe Journal of biological chemistryArticle
Corrections and comments
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Authors and funding
3 authors at 3 institutions in 1 country.
Funding
Abstract
The human hepatic organic cation transporter 1 (hOCT1) is a well-known transporter of both xenobiotic and endogenous cations. The substrates and inhibitors of hOCT1 are structurally and physiochemically diverse and include some widely prescribed drugs (metformin and imatinib), vitamins (thiamine), and neurotransmitters (serotonin). It has been demonstrated that the closely related renal isoform, hOCT2, is subject to ligand-dependent modulation, wherein one ligand may enhance or inhibit transport of a second, chemically unrelated, ligand. This phenomenon has important implications for drug-drug interactions due to the ubiquity of polypharmacy and the large number of drugs that are present as cations under physiological conditions. Therefore, the objective of this study was to determine if hOCT1 is subject to the same ligand-dependent modulation as hOCT2, and to identify unique putative ligand binding sites in the translocation channel for a sub-set of ligands using computational modeling. The competitive counter flow (CCF) assay was employed to examine ligand-dependent effects by utilizing four different radiolabeled probe substrates: MPP
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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.