ArticleScientific reports2012
Chemical structure of Retro-2, a compound that protects cells against ribosome-inactivating proteins.
Article in Scientific reports, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 33 citations in OpenAlex.
- Retrograde trafficking inhibitors allosterically trap Get3 to block tail-anchored protein biogenesis.bioRxiv : the preprint server for biology · 2026Article
- Biophysical and Biochemical Assays for Screening Small Molecule Inhibitors Targeting Toxin-Ribosome Interactions.Toxins · 2026Review
- The Search for Antidotes Against Ricin.Mini reviews in medicinal chemistry · 2024Review
- Halting ErbB-2 isoforms retrograde transport to the nucleus as a new theragnostic approach for triple-negative breast cancer.Cell death & disease · 2022Article
- Small Molecule Inhibitors Targeting the Interaction of Ricin Toxin A Subunit with Ribosomes.ACS infectious diseases · 2020Article
- Novel small molecule retrograde transport blocker confers post-exposure protection against ricin intoxication.Acta pharmaceutica Sinica. B · 2020Article
- Intracellular Neutralization of Ricin Toxin by Single-domain Antibodies Targeting the Active Site.Journal of molecular biology · 2020Article
- Article
- Intravesicular epidermal growth factor receptor subject to retrograde trafficking drives epidermal growth factor-dependent migration.Oncotarget · 2018Article
- Structurally optimized analogs of the retrograde trafficking inhibitor Retro-2cycl limit Leishmania infections.PLoS neglected tropical diseases · 2017Article
- Protection against Shiga Toxins.Toxins · 2017Review
- JC polyomavirus attachment, entry, and trafficking: unlocking the keys to a fatal infection.Journal of neurovirology · 2015Review
- Post-HTS case report and structural alert: Promiscuous 4-aroyl-1,5-disubstituted-3-hydroxy-2H-pyrrol-2-one actives verified by ALARM NMR.Bioorganic & medicinal chemistry letters · 2015Article
- Syntaxin 5-dependent retrograde transport to the trans-Golgi network is required for adeno-associated virus transduction.Journal of virology · 2015Article
- Structural optimization of a retrograde trafficking inhibitor that protects cells from infections by human polyoma- and papillomaviruses.Bioorganic & medicinal chemistry · 2014Article
- The essential roles of chemistry in high-throughput screening triage.Future medicinal chemistry · 2014Review
- (S)-N-Methyldihydroquinazolinones are the Active Enantiomers of Retro-2 Derived Compounds against Toxins.ACS medicinal chemistry letters · 2014Article
- Artificial photosynthesis of oxalate and oxalate-based polymer by a photovoltaic reactor.Scientific reports · 2014Article
- Common pharmacophore of structurally distinct small-molecule inhibitors of intracellular retrograde trafficking of ribosome inactivating proteins.Scientific reports · 2013Article
- Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
Abstract
Shiga-like toxins and ricin are ribosome-inactivating proteins (RIPs) that are lethal to mammals and pose a global health threat. No clinical vaccines or therapeutics currently exist to protect against these RIPs. Two small molecules (Retro-1 and Retro-2) were discovered with high-throughput screening and reported for their protection of cells against RIPs. Of great significance, Retro-2, reported as (E)-2-(((5-methylthiophen-2-yl)methylene)amino)-N-phenylbenzamide, fully protected mice from lethal nasal challenge with ricin. Herein, we report studies showing that the chemical structure of Retro-2 is (±)-2-(5-methylthiophen-2-yl)-3-phenyl-2,3-dihydroquinazolin-4(1H)-one rather than (E)-2-(((5-methylthiophen-2-yl)methylene)amino)-N-phenylbenzamide. The latter is an achiral molecule that converts spontaneously to the former, which is a racemate and showed cell protection against RIPs. This calls for attention to (±)-2-(5-methylthiophen-2-yl)-3-phenyl-2,3-dihydroquinazolin-4(1H)-one as a promising RIP inhibitor and for chemical characterization of drug leads obtained from high-throughput screens.
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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.