https://nova.newcastle.edu.au/vital/access/ /manager/Index ${session.getAttribute("locale")} 5 The rhodadyns, a new class of small molecule inhibitors of dynamin GTPase activity https://nova.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://nova.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 ]]> Azido and diazarinyl analogues of bis-tyrphostin as asymmetrical inhibitors of dynamin GTPase https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:8246 Sat 24 Mar 2018 08:40:38 AEDT ]]> Inhibition of dynamin mediated endocytosis by the dynoles-synthesis and functional activity of a family of indoles https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:8338 Sat 24 Mar 2018 08:37:03 AEDT ]]> Iminochromene inhibitors of Dynamins I and II GTPase activity and Endocytosis https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:11334 Sat 24 Mar 2018 08:13:29 AEDT ]]> The dynamin inhibitors MiTMAB and OcTMAB induce cytokinesis failure and inhibit cell proliferation in human cancer cells https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:11336 Sat 24 Mar 2018 08:13:29 AEDT ]]> The Pthaladyns: GTP competitive inhibitors of Dynamin I and II GTPase derived from virtual screening https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:10254 Sat 24 Mar 2018 08:13:07 AEDT ]]> Inhibition of dynamin by dynole 34-2 induces cell death following cytokinesis failure in cancer cells https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:17425 Sat 24 Mar 2018 08:01:39 AEDT ]]> Dynamin inhibition blocks botulinum neurotoxin type A endocytosis in neurons and delays botulism https://nova.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 ]]> Pyrimidyn compounds: dual-action small molecule pyrimidine-based dynamin inhibitors https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:19893 Sat 24 Mar 2018 07:57:02 AEDT ]]> Development of second-generation indole-based dynamin GTPase inhibitors https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:20159 Sat 24 Mar 2018 07:51:36 AEDT ]]> 1,8-Naphthalimide derivatives: new leads against dynamin i GTPase activity https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:23187 50 of 19.1 ± 0.3 and 18.5 ± 1.7 μM respectively). Compound 29 showed effective inhibition of clathrin-mediated endocytosis (IC50(CME) 66 μM). The results introduce 29 as an optimised GTP-competitive lead Naphthaladyn™ compound for the further development of naphthalimide-based dynI GTPase inhibitors.]]> Sat 24 Mar 2018 07:10:29 AEDT ]]>