ArticleChemical science2020
Inhibitors of thiol-mediated uptake.
Article in Chemical science, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
24 citing papers in PubMed, 57 citations in OpenAlex.
- The Effect of Ligand Reactivity and Carrier Mechanics on Thiol-Mediated Cellular Uptake for miRNA Nano-Drugs.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Peptide/Protein Functionalization and Macrocyclization via Alkyne Umpolung with Hypervalent Iodine Reagents.Accounts of chemical research · 2025Article
- Medical and Nonmedical Applications of Synthetic Transmembrane Anion Transporters.Chemical reviews · 2025Review
- Site-Specific Disulfide-Mediated Crosslinking of DNA Nanocubes for Enhanced Biological Applications.Small science · 2025Article
- Mechanistic Insights into the Tools for Intracellular Protein Delivery.Chem & bio engineering · 2025Review
- Photochemical Stabilization of Self-Assembled Spherical Nucleic Acids.Small (Weinheim an der Bergstrasse, Germany) · 2025Article
- Pentathiepins are an understudied molecular prism of biological activities.Archiv der Pharmazie · 2024Review
- Inclusive Pattern Generation Protocols to Decode Thiol-Mediated Uptake.ACS central science · 2024Article
- Article
- Synthesis of Seven Indolizine-Derived Pentathiepines: Strong Electronic Structure Response to Nitro Substitution in Position C-9.Molecules (Basel, Switzerland) · 2023Article
- FluorogenicJACS Au · 2023Article
- IMT504 protects beta cells against apoptosis and maintains beta cell identity, without modifying proliferation.Physiological reports · 2023Article
- Article
- Dynamic Covalent Michael Acceptors to Penetrate Cells: Thiol-Mediated Uptake with Tetrel-Centered Exchange Cascades, Assisted by Halogen-Bonding Switches.Angewandte Chemie (International ed. in English) · 2022Article
- Beyond the vaccines: a glance at the small molecule and peptide-based anti-COVID19 arsenal.Journal of biomedical science · 2022Review
- Gastrointestinal Tract Stabilized Protein Delivery Using Disulfide Thermostable Exoshell System.International journal of molecular sciences · 2022Article
- Article
- Cyclic Thiosulfonates for Thiol-Mediated Uptake: Cascade Exchangers, Transporters, Inhibitors.JACS Au · 2022Article
- Cyclic 5-membered disulfides are not selective substrates of thioredoxin reductase, but are opened nonspecifically.Nature communications · 2022Article
- Recent advances in developing small-molecule inhibitors against SARS-CoV-2.Acta pharmaceutica Sinica. B · 2022Review
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Ellman's reagent has caused substantial confusion and concern as a probe for thiol-mediated uptake because it is the only established inhibitor available but works neither efficiently nor reliably. Here we use fluorescent cyclic oligochalcogenides that enter cells by thiol-mediated uptake to systematically screen for more potent inhibitors, including epidithiodiketopiperazines, benzopolysulfanes, disulfide-bridged γ-turned peptides, heteroaromatic sulfones and cyclic thiosulfonates, thiosulfinates and disulfides. With nanomolar activity, the best inhibitors identified are more than 5000 times better than Ellman's reagent. Different activities found with different reporters reveal thiol-mediated uptake as a complex multitarget process. Preliminary results on the inhibition of the cellular uptake of pseudo-lentivectors expressing SARS-CoV-2 spike protein do not exclude potential of efficient inhibitors of thiol-mediated uptake for the development of new antivirals.
Identifiers
What OpenQuestion holds
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.