Dynasore

Background

Dynasore is a cell-permeable, small-molecule inhibitor of the endocytosis-associated GTPase dynamin (IC₅₀ = 15 mM). Dynamin promotes clathrin-coated vesicle formation and is involved in detaching coated pits from the membrane during clathrin-mediated endocytosis. Dynasore inhibits the GTPase activity of dynamin I, dynamin II, dynamin-related protein 1, and mitochondrial dynamin. By blocking dynamin, Dynasore inhibits coated vesicle formation and dynamin-mediated endocytic pathways (1). In a study of hippocampal synapses, inhibition by Dynasore demonstrated that dynamin is essential for all forms of synaptic vesicle endocytosis, and that Dynasore has no effect on exocytosis (2). A study of hepatocellular carcinoma demonstrated that Dynasore enhanced the inhibitory effects of c-Met inhibitors on hepatoma cell proliferation and migration, and led to increased cell cycle arrest and apoptosis (3). Dynasore blocked HSV-1 entry into human and murine keratinocytes, and prevented HSV-1 and HSV-2 infection of human epithelial and neuronal cells, including primary genital tract cells and human fetal neurons and astrocytes (4).