https://ogma.newcastle.edu.au/vital/access/ /manager/Index ${session.getAttribute("locale")} 5 Clathrin-independent carriers form a high capacity endocytic sorting system at the leading edge of migrating cells https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:10991 Wed 11 Apr 2018 14:47:28 AEST ]]> The rhodadyns, a new class of small molecule inhibitors of dynamin GTPase activity https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:21743 50 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.]]> Wed 02 Dec 2015 10:02:08 AEDT ]]> Building a better dynasore: the Dyngo compounds potently inhibit dynamin and endocytosis https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:20160 36-fold reduced activity against rings, suggesting that they can discriminate between helical or ring oligomerization states. 4a and 6a inhibited dynamin-dependent endocytosis of transferrin in multiple cell types (IC50 of 5.7 and 5.8 μM, respectively), at least sixfold more potently than dynasore, but had no effect on dynamin-independent endocytosis of cholera toxin. 4a also reduced synaptic vesicle endocytosis and activity-dependent bulk endocytosis in cultured neurons and synaptosomes. Overall, 4a and 6a are improved and versatile helical dynamin and endocytosis inhibitors in terms of potency, non-specific binding and cytotoxicity. The data further suggest that the ring oligomerization state of dynamin is not required for clathrin-mediated endocytosis.]]> Tue 24 Aug 2021 14:23:34 AEST ]]> Dynamin inhibition blocks botulinum neurotoxin type A endocytosis in neurons and delays botulism https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:17423 TM, was sufficient to abolish BoNT/A-Hc internalization and BoNT/A-induced SNAP25 cleavage in hippocampal neurons. Dyngo-4a also interfered with BoNT/A-Hc internalization into motor nerve terminals. Furthermore, Dyngo-4a afforded protection against BoNT/A-induced paralysis at the rat hemidiaphragm. A significant delay of >30% in the onset of botulism was observed in mice injected with Dyngo-4a. Dynamin inhibition therefore provides a therapeutic avenue for the treatment of botulism and other diseases caused by pathogens sharing dynamin-dependent uptake mechanisms.]]> Sat 24 Mar 2018 08:01:38 AEDT ]]>