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Updated: Apr 28, 2026

Detection of Small GTPase Prenylation and GTP Binding Using Membrane Fractionation and GTPase-linked Immunosorbent Assay
Published on: November 11, 2018
The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity
Mark J Robertson1, Gordana Hadzic1, Joseph Ambrus1
1Chemistry, The University of Newcastle , University Drive, Callaghan, NSW 2308, Australia.
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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