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

被引：368

作者：

Kirchhausen, Tom ^{[1
,2
]}

Macia, Eric ^{[1
,2
,4
]}

Pelish, Henry E. ^{[1
,2
,3
]}

机构：

[1] Harvard Univ, Sch Med, Dept Cell Biol, Boston, MA 02115 USA

[2] IDI Immune Res Inst, Boston, MA USA

[3] Makoto Life Sci Inc, Boston, MA USA

[4] CNRS, Inst Pharmacol Mol & Cellulaire, F-06560 Valbonne, France

来源：

SMALL GTPASES IN DISEASE, PART A | 2008年 / 438卷

关键词：

D O I：

10.1016/S0076-6879(07)38006-3

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

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 similar to 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.

引用

页码：77 / 93

页数：17

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