ArticleACS medicinal chemistry letters2012
The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity.
Article in ACS medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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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.
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Who cites it
12 citing papers in PubMed, 43 citations in OpenAlex.
- The Chemical Inhibitors of Endocytosis: From Mechanisms to Potential Clinical Applications.Cells · 2023Review
- The sulfonadyns: a class of aryl sulfonamides inhibiting dynamin I GTPase and clathrin mediated endocytosis are anti-seizure in animal models.RSC medicinal chemistry · 2023Article
- Mechanistic-Based Classification of Endocytosis-Related Inhibitors: Does It Aid in Assigning Drugs against SARS-CoV-2?Viruses · 2023Review
- Insight into the role of clathrin-mediated endocytosis inhibitors in SARS-CoV-2 infection.Reviews in medical virology · 2023Review
- Prodrugs of the Archetypal Dynamin Inhibitor Bis-T-22.ChemMedChem · 2022Article
- Role of Clathrin and Dynamin in Clathrin Mediated Endocytosis/Synaptic Vesicle Recycling and Implications in Neurological Diseases.Frontiers in cellular neuroscience · 2021Review
- Measuring Endocytosis During Proliferative Cell Quiescence.Methods in molecular biology (Clifton, N.J.) · 2021Article
- Synthesis of the Pitstop family of clathrin inhibitors.Nature protocols · 2014Article
- Synthesis of Dynole 34-2, Dynole 2-24 and Dyngo 4a for investigating dynamin GTPase.Nature protocols · 2014Article
- The significance of dynamin 2 expression for prostate cancer progression, prognostication, and therapeutic targeting.Cancer medicine · 2014Article
- Building a better dynasore: the dyngo compounds potently inhibit dynamin and endocytosis.Traffic (Copenhagen, Denmark) · 2013Article
- A simple and green procedure for the synthesis of 5-arylidenerhodanines catalyzed by diammonium hydrogen phosphate in water.TheScientificWorldJournal · 2013Article
Corrections and comments
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Authors and funding
12 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Six focused rhodanine-based libraries, 60 compounds in total, were synthesized and evaluated as potential dynamin I GTPase inhibitors. Twenty-six were more potent than the lead compound with 13 returning IC50 values ≤10 μM, making the Rhodadyn series among the most active dynamin inhibitors reported. Two analogues were highly effective at blocking receptor-mediated endocytosis: C10 and D10 with IC50(RME) = 7.0 ± 2.2 and 5.9 ± 1.0 μM, respectively. These compounds are equipotent with the best reported in-cell dynamin inhibitors.
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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.