ArticleACS medicinal chemistry letters2014
(S)-N-Methyldihydroquinazolinones are the Active Enantiomers of Retro-2 Derived Compounds against Toxins.
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Endocytosis and Endocytic Neurotrophin Signaling in Developing Spiral Ganglion Neurons.International journal of molecular sciences · 2026Article
- Retrograde trafficking inhibitors allosterically trap Get3 to block tail-anchored protein biogenesis.bioRxiv : the preprint server for biology · 2026Article
- Article
- In Vivo Sustained Release of the Retrograde Transport Inhibitor Retro-2.1 Formulated in a Thermosensitive Hydrogel.International journal of molecular sciences · 2022Article
- Halting ErbB-2 isoforms retrograde transport to the nucleus as a new theragnostic approach for triple-negative breast cancer.Cell death & disease · 2022Article
- The Cellular and Chemical Biology of Endocytic Trafficking and Intracellular Delivery-The GL-Lect Hypothesis.Molecules (Basel, Switzerland) · 2021Review
- Identification of an Antiviral Compound from the Pandemic Response Box that Efficiently Inhibits SARS-CoV-2 Infection In Vitro.Microorganisms · 2020Article
- Shiga Toxin Uptake and Sequestration in Extracellular Vesicles Is Mediated by Its B-Subunit.Toxins · 2020Article
- Targeting the Early Endosome-to-Golgi Transport of Shiga Toxins as a Therapeutic Strategy.Toxins · 2020Review
- Functional dissection of the retrograde Shiga toxin trafficking inhibitor Retro-2.Nature chemical biology · 2020Article
- Small Trafficking Inhibitor Retro-2 Disrupts the Microtubule-Dependent Trafficking of Autophagic Vacuoles.Frontiers in cell and developmental biology · 2020Article
- Shiga Toxin-Bearing Microvesicles Exert a Cytotoxic Effect on Recipient Cells Only When the Cells Express the Toxin Receptor.Frontiers in cellular and infection microbiology · 2020Article
- Inhibition of diverse opportunistic viruses by structurally optimized retrograde trafficking inhibitors.Bioorganic & medicinal chemistry · 2019Article
- Article
- Structurally optimized analogs of the retrograde trafficking inhibitor Retro-2cycl limit Leishmania infections.PLoS neglected tropical diseases · 2017Article
- Protection against Shiga Toxins.Toxins · 2017Review
- Potent Inhibition of Human Cytomegalovirus by Modulation of Cellular SNARE Syntaxin 5.Journal of virology · 2017Article
- Vaccinia Virus Uses Retromer-Independent Cellular Retrograde Transport Pathways To Facilitate the Wrapping of Intracellular Mature Virions during Virus Morphogenesis.Journal of virology · 2016Article
- Retrograde Transport from Early Endosomes to the trans-Golgi Network Enables Membrane Wrapping and Egress of Vaccinia Virus Virions.Journal of virology · 2016Article
- Syntaxin 5-dependent retrograde transport to the trans-Golgi network is required for adeno-associated virus transduction.Journal of virology · 2015Article
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
This study reports the synthesis, chromatographic separation, and pharmacological evaluation of the two enantiomers of a new compound, named Retro-2.1, active against toxins by inhibiting intracellular trafficking via the retrograde route. The absolute configuration of the bioactive enantiomer has been assigned from X-ray diffraction to the (S)-enantiomer. To date, (S)-Retro-2.1 is the most potent molecule to counteract the cytotoxic potential of ricin and Shiga toxin, with EC50 values of 23 and 54 nM, respectively.
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