https://nova.newcastle.edu.au/vital/access/ /manager/Index ${session.getAttribute("locale")} 5 Pyrimidine-based inhibitors of dynamin I GTPase activity: competitive inhibition at the pleckstrin homology domain https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:32119 (CME) = 65.9 ± 7.7 to 3.7 ± 1.1 mM), which makes this series among the more potent inhibitors of dynamin and CME yet reported. In CME and growth inhibition cell-based assays, the data obtained was consistent with dynamin inhibition. CEREP ExpresS profiling identified off-target effects at the cholecystokinin, dopamine D₂, histamine H₁ and H₂, melanocortin, melatonin, muscarinic M₁ and M₃, neurokinin, opioid KOP and serotonin receptors.]]> Thu 03 May 2018 12:18:53 AEST ]]> 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 ]]> Synthesis of dynole 34-2, dynole 2-24 and dyngo 4a for investigating dynamin GTPase https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:21262 Sat 24 Mar 2018 07:54:43 AEDT ]]> Dynamin regulates specific membrane fusion events necessary for acrosomal exocytosis in mouse spermatozoa https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:22263 in vitro induction of acrosomal exocytosis by progesterone, but not by the calcium ionophore A23187, and elicited a concomitant reduction of in vitro fertilization. In vivo treatment with these inhibitors also resulted in spermatozoa displaying reduced acrosome reaction potential. Dynamin 1 and 2 phosphorylation increased on progesterone treatment, and this was also selectively blocked by dynasore. On the basis of our collective data, we propose that dynamin could regulate specific membrane fusion events necessary for acrosomal exocytosis in mouse spermatozoa.]]> Sat 24 Mar 2018 07:17:38 AEDT ]]>