Use of dynasore, the small molecule inhibitor of dynamin, in the regulation of endocytosis.
Methods Enzymol
; 438: 77-93, 2008.
Article
em En
| MEDLINE
| ID: mdl-18413242
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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Dinaminas
/
Hidrazonas
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Methods Enzymol
Ano de publicação:
2008
Tipo de documento:
Article
País de afiliação:
Estados Unidos