ArticleNature structural & molecular biology2019
Structures of human ENT1 in complex with adenosine reuptake inhibitors.
Article in Nature structural & molecular biology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 65 papers.
What it found
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Who cites it
65 citing papers in PubMed, 63 citations in OpenAlex.
- The SLC-ome of membrane transport: from molecular discovery to physiology and clinical applications.Physiological reviews · 2026Review
- Identification of Putative Equilibrative Nucleoside Transporter Inhibitors Through Dual-Pharmacophore Virtual Screening and Validation in a Gemcitabine-Based Cell Assay.Molecules (Basel, Switzerland) · 2026Article
- Tailored for swift recognition: A structural perspective on secondary active plant hormone transporters.The Plant journal : for cell and molecular biology · 2026Review
- Article
- Calponin-3 is associated with epilepsy through the regulation of astrocyte activity.Brain pathology (Zurich, Switzerland) · 2026Article
- Anti-Toxoplasma activity of NBMPR is mediated through the inhibition of nucleoside and nucleobase transporters.Parasitology research · 2026Article
- Membrane transport of root-borne trans-zeatin riboside maintains the cytokinin homeostasis in shoots.Journal of experimental botany · 2025Article
- Article
- Preclinical Evaluation of a Novel Molecule Targeting Nucleoside Homeostasis to Restore Energy Metabolism and Cognitive Function in Alzheimer's Disease.Pharmacology research & perspectives · 2025Article
- ENT-1-Targeted Polymersomes to Enhance the Efficacy of Methotrexate in Choriocarcinoma Treatment.Small science · 2025Article
- Molecular basis of the urate transporter URAT1 inhibition by gout drugs.Nature communications · 2025Article
- Cross-tissue coordination between SLC nucleoside transporters regulates reproduction in Caenorhabditis elegans.PLoS genetics · 2025Article
- Structure and transport mechanism of human riboflavin transporters.Nature communications · 2025Article
- Exploring novel dilazep derivatives as hENT1 inhibitors and potentially covalent molecular tools.Purinergic signalling · 2025Article
- SLC29A1 and SLC29A2 are human nicotinamide cell membrane transporters.Nature communications · 2025Article
- Landscape of targets within nucleoside metabolism for the modification of immune responses.Frontiers in oncology · 2025Review
- Design of an equilibrative nucleoside transporter subtype 1 inhibitor for pain relief.Nature communications · 2024Article
- The JNK Signaling Pathway Regulates Seizures Through ENT1 in Pilocarpine-Induced Epilepsy Rat Model.CNS neuroscience & therapeutics · 2024Article
- ATP-Binding Cassette and Solute Carrier Transporters: Understanding Their Mechanisms and Drug Modulation Through Structural and Modeling Approaches.Pharmaceuticals (Basel, Switzerland) · 2024Review
- A proteome-wide structural systems approach reveals insights into protein families of all human herpesviruses.Nature communications · 2024Article
5 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
Abstract
The human equilibrative nucleoside transporter 1 (hENT1), a member of the SLC29 family, plays crucial roles in adenosine signaling, cellular uptake of nucleoside for DNA and RNA synthesis, and nucleoside-derived anticancer and antiviral drug transport in humans. Because of its central role in adenosine signaling, it is the target of adenosine reuptake inhibitors (AdoRI), several of which are used clinically. Despite its importance in human physiology and pharmacology, the molecular basis of hENT1-mediated adenosine transport and its inhibition by AdoRIs are limited, owing to the absence of structural information on hENT1. Here, we present crystal structures of hENT1 in complex with two chemically distinct AdoRIs: dilazep and S-(4-nitrobenzyl)-6-thioinosine (NBMPR). Combined with mutagenesis study, our structural analyses elucidate two distinct inhibitory mechanisms exhibited on hENT1 and provide insight into adenosine recognition and transport. Our studies provide a platform for improved pharmacological intervention of adenosine and nucleoside analog drug transport by hENT1.
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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.