Dynamin

Dynamin inhibitors block the large GTPase that pinches endocytic vesicles off the plasma membrane. Dynamin assembles as a helical collar around the neck of budding clathrin-coated pits and uses guanosine triphosphate (GTP) hydrolysis to drive membrane fission. Mammals express dynamin 1 in neurons, dynamin 2 in most tissues and dynamin 3 mainly in brain and testis. Dynasore, described in 2006 as a cell-permeable inhibitor, blocks dynamin GTPase activity and rapidly stops endocytosis. Dyngo-4a and Dynole 34-2 are later dynamin inhibitors used in studies of synaptic vesicle recycling and receptor internalization. Mdivi-1 was reported in 2008 to inhibit the dynamin-related protein that divides mitochondria, dynamin-related protein 1 (DRP1) in mammals.

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