ArticleInternational journal of molecular sciences2018
Discovery of Potent Inhibitors for the Large Neutral Amino Acid Transporter 1 (LAT1) by Structure-Based Methods.
Article in International journal of molecular sciences, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
What it found
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Who cites it
32 citing papers in PubMed.
- Quantitative single cell analysis of gold nanoparticle association across a mouse triple-negative breast cancer cell line and blood immune cell populations.Analytical and bioanalytical chemistry · 2026Article
- Dysregulation of the urea cycle - potential targets for treatment and diagnosis in prostate cancer.Expert reviews in molecular medicine · 2026Review
- A LAT1-Compatible, Leadlike Tyrosine-Naphthoquinone Conjugate With Anticancer Activity.Drug development research · 2026Article
- Sustained reductions in valine and isoleucine mediate anti-cancer pharmacological effects of inhibiting amino acid transporter LAT1 in cancer cells.Cancer & metabolism · 2025Article
- D-alanine synthesis and exogenous alanine affect the antimicrobial susceptibility ofAntimicrobial agents and chemotherapy · 2025Article
- SLC7 transporters at the crossroads of amino acid metabolism and diabetes pathophysiology: insights and therapeutic perspectives.Frontiers in nutrition · 2025Review
- LAT1-specific PET radiotracers: Development and clinical experiences of a new class of cancer-specific radiopharmaceuticals.Theranostics · 2025Review
- Synthesis, Cytotoxicity, and Mechanistic Evaluation of Tetrahydrocurcumin-Amino Acid Conjugates as LAT1-Targeting Anticancer Agents in C6 Glioma Cells.International journal of molecular sciences · 2024Article
- Photoredox-Catalyzed Generation of Tertiary Anions from Primary Amines via a Radical Polar Crossover.Angewandte Chemie (International ed. in English) · 2024Article
- Exploring Amino Acid Transporters as Therapeutic Targets for Cancer: An Examination of Inhibitor Structures, Selectivity Issues, and Discovery Approaches.Pharmaceutics · 2024Review
- Investigation of effects of transferrin-conjugated gold nanoparticles on hippocampal neuronal activity and anxiety behavior in mice.Molecular and cellular biochemistry · 2023Article
- Characterization of substrates and inhibitors of the human heterodimeric transporter 4F2hc-LAT1 using purified protein and the scintillation proximity radioligand binding assay.Frontiers in physiology · 2023Article
- Describing inhibitor specificity for the amino acid transporter LAT1 from metainference simulations.Biophysical journal · 2022Article
- Pharmacologic inhibition of LAT1 predominantly suppresses transport of large neutral amino acids and downregulates global translation in cancer cells.Journal of cellular and molecular medicine · 2022Article
- The Evaluation of l-Tryptophan Derivatives as Inhibitors of the l-Type Amino Acid Transporter LAT1 (SLC7A5).ChemMedChem · 2022Article
- Impact of Inhibition of Glutamine and Alanine Transport on Cerebellar Glial and Neuronal Metabolism.Biomolecules · 2022Article
- Transport of Biologically Active Ultrashort Peptides Using POT and LAT Carriers.International journal of molecular sciences · 2022Review
- Cysteine Donor-Based Brain-Targeting Prodrug: Opportunities and Challenges.Oxidative medicine and cellular longevity · 2022Review
- Rush Hour of LATs towards Their Transport Cycle.Membranes · 2021Review
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Authors and funding
8 authors.
Funding
Abstract
The large neutral amino acid transporter 1 (LAT1) is a promising anticancer target that is required for the cellular uptake of essential amino acids that serve as building blocks for cancer growth and proliferation. Here, we report a structure-based approach to identify chemically diverse and potent inhibitors of LAT1. First, a homology model of LAT1 that is based on the atomic structures of the prokaryotic homologs was constructed. Molecular docking of nitrogen mustards (NMs) with a wide range of affinity allowed for deriving a common binding mode that could explain the structure-activity relationship pattern in NMs. Subsequently, validated binding hypotheses were subjected to molecular dynamics simulation, which allowed for extracting a set of dynamic pharmacophores. Finally, a library of ~1.1 million molecules was virtually screened against these pharmacophores, followed by docking. Biological testing of the 30 top-ranked hits revealed 13 actives, with the best compound showing an IC
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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.