ArticleJournal of medicinal chemistry2015
A binding mode hypothesis of tiagabine confirms liothyronine effect on γ-aminobutyric acid transporter 1 (GAT1).
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 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
18 citing papers in PubMed.
- Careful Examination of a Novel Azobenzene Paroxetine Derivative and Its Interactions With Biogenic Amine Transporters.Journal of neurochemistry · 2025Article
- Article
- Visualizing GABA transporters in vivo: an overview of reported radioligands and future directions.EJNMMI research · 2023Review
- A comparative review on the well-studied GAT1 and the understudied BGT-1 in the brain.Frontiers in physiology · 2023Review
- Article
- Structural insights into GABA transport inhibition using an engineered neurotransmitter transporter.The EMBO journal · 2022Article
- Structural basis of GABA reuptake inhibition.Nature · 2022Article
- Article
- Novel Functionalized Amino Acids as Inhibitors of GABA Transporters with Analgesic Activity.ACS chemical neuroscience · 2021Article
- Molecular Determinants and Pharmacological Analysis for a Class of Competitive Non-transported Bicyclic Inhibitors of the Betaine/GABA Transporter BGT1.Frontiers in chemistry · 2021Article
- Molecular Dynamic Simulations to Probe Stereoselectivity of Tiagabine Binding with Human GAT1.Molecules (Basel, Switzerland) · 2020Article
- Computational Dissection of Membrane Transport at a Microscopic Level.Trends in biochemical sciences · 2020Review
- Article
- Modeling and Simulation ofComputational and structural biotechnology journal · 2019Article
- Discovery of Potent Inhibitors for the Large Neutral Amino Acid Transporter 1 (LAT1) by Structure-Based Methods.International journal of molecular sciences · 2018Article
- Article
- Empowering pharmacoinformatics by linked life science data.Journal of computer-aided molecular design · 2017Article
- SLC Transporters: Structure, Function, and Drug Discovery.MedChemComm · 2016Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
Elevating GABA levels in the synaptic cleft by inhibiting its reuptake carrier GAT1 is an established approach for the treatment of CNS disorders like epilepsy. With the increasing availability of crystal structures of transmembrane transporters, structure-based approaches to elucidate the molecular basis of ligand-transporter interaction also become feasible. Experimental data guided docking of derivatives of the GAT1 inhibitor tiagabine into a protein homology model of GAT1 allowed derivation of a common binding mode for this class of inhibitors that is able to account for the distinct structure-activity relationship pattern of the data set. Translating essential binding features into a pharmacophore model followed by in silico screening of the DrugBank identified liothyronine as a drug potentially exerting a similar effect on GAT1. Experimental testing further confirmed the GAT1 inhibiting properties of this thyroid hormone.
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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.