Dynamin is a large, 100kDa, GTPase that is able (required) to assemble into rings comprising 26-32 tetrameric units and into helices representing the assembly of 100’s to 1000’s of dynamin monomers. In these macromolecular assemblies the GTPase activity of dynamin is massively stimulated. Dynamin has two primary roles: a role in the final stages of clathrin mediated endocytosis where it is responsible for the release of the clathrin coated vesicle from the plasma membrane; and a role in mitosis (final stages of cell division) where dynamin is involved in the cleavage of the intracellular bridge. The hydrolysis of GTP to GDP by dynamin supplies the energy required for both of these processes.
This presentation will explore some of our efforts to “streamline a dynamin drug development pathway” and the discovery of novel molecules that affect the stability of dynamins macromolecular structures and the identification of potential new biological roles for dynamin in vivo.