| Use of dynasore, the small molecule inhibitor of dynamin, in the regulation of endocytosis. | |
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MedLine Citation:
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PMID: 18413242 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Tom Kirchhausen; Eric Macia; Henry E Pelish |
Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural |
Journal Detail:
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Title: Methods in enzymology Volume: 438 ISSN: 0076-6879 ISO Abbreviation: Meth. Enzymol. Publication Date: 2008 |
Date Detail:
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Created Date: 2008-04-16 Completed Date: 2008-06-19 Revised Date: 2012-10-09 |
Medline Journal Info:
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Nlm Unique ID: 0212271 Medline TA: Methods Enzymol Country: United States |
Other Details:
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Languages: eng Pagination: 77-93 Citation Subset: IM |
Affiliation:
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Department of Cell Biology, Harvard Medical School, and IDI Immune Research Institute, Boston, Massachusetts, USA. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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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:
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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; R01 GM075252-06/GM/NIGMS NIH HHS |
| Chemical | |
Reg. No./Substance:
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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 | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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