Document Detail


Use of dynasore, the small molecule inhibitor of dynamin, in the regulation of endocytosis.
MedLine Citation:
PMID:  18413242     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Tom Kirchhausen; Eric Macia; Henry E Pelish
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural    
Journal Detail:
Title:  Methods in enzymology     Volume:  438     ISSN:  0076-6879     ISO Abbreviation:  Meth. Enzymol.     Publication Date:  2008  
Date Detail:
Created Date:  2008-04-16     Completed Date:  2008-06-19     Revised Date:  2014-09-17    
Medline Journal Info:
Nlm Unique ID:  0212271     Medline TA:  Methods Enzymol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  77-93     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Cytoskeleton / drug effects
Dynamin II / antagonists & inhibitors
Dynamins / analysis,  antagonists & inhibitors*
Endocytosis
Humans
Hydrazones / pharmacology*
Protein Transport / drug effects
Spodoptera
Grant Support
ID/Acronym/Agency:
GM03548/GM/NIGMS NIH HHS; GM075252/GM/NIGMS NIH HHS; GM62566/GM/NIGMS NIH HHS; R01 GM036548/GM/NIGMS NIH HHS; R01 GM075252/GM/NIGMS NIH HHS; R01 GM075252-04/GM/NIGMS NIH HHS
Chemical
Reg. No./Substance:
0/Hydrazones; 0/N'-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthahydrazide; EC 3.6.5.5/Dynamin II; EC 3.6.5.5/Dynamins
Comments/Corrections

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