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Methods Enzymol. 2008;438:77-93. doi: 10.1016/S0076-6879(07)38006-3.

Use of dynasore, the small molecule inhibitor of dynamin, in the regulation of endocytosis.

Author information

1
Department of Cell Biology, Harvard Medical School, and IDI Immune Research Institute, Boston, Massachusetts, USA.

Abstract

The large GTPase dynamin is essential for clathrin-dependent coated-vesicle formation. Dynasore is a cell-permeable small molecule that inhibits the GTPase activity of dynamin1, dynamin2 and Drp1, the mitochondrial dynamin. Dynasore was discovered in a screen of approximately 16,000 compounds for inhibitors of the dynamin2 GTPase. Dynasore is a noncompetitive inhibitor of dynamin GTPase activity and blocks dynamin-dependent endocytosis in cells, including neurons. It is fast acting (seconds) and its inhibitory effect in cells can be reversed by washout. Here we present a detailed synthesis protocol for dynasore, and describe a series of experiments used to analyze the inhibitory effects of dynasore on dynamin in vitro and to study the effects of dynasore on endocytosis in cells.

PMID:
18413242
PMCID:
PMC2796620
DOI:
10.1016/S0076-6879(07)38006-3
[Indexed for MEDLINE]
Free PMC Article

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