Dynamin Inhibitors

It is likely that a pharmaceutical approach that controls the activity of dynamin in the brain may provide a new therapy for human brain disorders of synaptic transmission.  In collaboration with Medicinal Chemistry at the University of Newcastle, we are actively pursuing a program to design such compounds.  We have developed several lead compounds that block dynamin’s GTPase activityin vitro.  These drugs abolish endocytosis in neurons, providing a new point of control over the process.  We are currently producing pro-drugs that greatly improve their entry into cells.  These pro-drugs have no inhibitory activity, but are activated in the body by cellular esterases.  We created several pro-drugs that will greatly increase the half-life of the drug in living tissue, hence improving the drugs effectiveness and efficiency when administered to animals.  The development of anti-dynamin drugs could lead to better targeted antiepileptic and anticancer drugs.