{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,7]],"date-time":"2026-10-07T03:15:53Z","timestamp":1791342953712,"version":"4.3.1"},"reference-count":64,"publisher":"Wiley","issue":"12","license":[{"start":{"date-parts":[[2013,10,9]],"date-time":"2013-10-09T00:00:00Z","timestamp":1381276800000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/3.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Traffic"],"published-print":{"date-parts":[[2013,12]]},"abstract":"<jats:p>\n                    <jats:bold>\n                      Dynamin\n                      <jats:styled-content style=\"fixed-case\">GTPase<\/jats:styled-content>\n                      activity increases when it oligomerizes either into helices in the presence of lipid templates or into rings in the presence of\n                      <jats:styled-content style=\"fixed-case\">SH3<\/jats:styled-content>\n                      domain proteins. Dynasore is a dynamin inhibitor of moderate potency (\n                      <jats:styled-content style=\"fixed-case\">\n                        IC\n                        <jats:sub>50<\/jats:sub>\n                      <\/jats:styled-content>\n                      \u02dc 15\u2009\u03bcM\n                      <jats:italic>in vitro<\/jats:italic>\n                      ). We show that dynasore binds stoichiometrically to detergents used for\n                      <jats:italic>in vitro<\/jats:italic>\n                      drug screening, drastically reducing its potency (\n                      <jats:styled-content style=\"fixed-case\">\n                        IC\n                        <jats:sub>50<\/jats:sub>\n                      <\/jats:styled-content>\n                      = 479\u2009\u03bcM) and research tool utility. We synthesized a focused set of dihydroxyl and trihydroxyl dynasore analogs called the\n                      <jats:styled-content style=\"fixed-case\">Dyngo\u2122<\/jats:styled-content>\n                      compounds, five of which had improved potency, reduced detergent binding and reduced cytotoxicity, conferred by changes in the position and\/or number of hydroxyl substituents. The Dyngo compound 4a was the most potent compound, exhibiting a 37\u2010fold improvement in potency over dynasore for liposome\u2010stimulated helical dynamin activity. In contrast, while dynasore about equally inhibited dynamin assembled in its helical or ring states, 4a and 6a exhibited &gt;36\u2010fold reduced activity against rings, suggesting that they can discriminate between helical or ring oligomerization states. 4a and 6a inhibited dynamin\u2010dependent endocytosis of transferrin in multiple cell types (\n                      <jats:styled-content style=\"fixed-case\">\n                        IC\n                        <jats:sub>50<\/jats:sub>\n                      <\/jats:styled-content>\n                      of 5.7 and 5.8\u2009\u03bcM, respectively), at least sixfold more potently than dynasore, but had no effect on dynamin\u2010independent endocytosis of cholera toxin. 4a also reduced synaptic vesicle endocytosis and activity\u2010dependent bulk endocytosis in cultured neurons and synaptosomes. Overall, 4a and 6a are improved and versatile helical dynamin and endocytosis inhibitors in terms of potency, non\u2010specific binding and cytotoxicity. The data further suggest that the ring oligomerization state of dynamin is not required for clathrin\u2010mediated endocytosis\n                    <\/jats:bold>\n                    .\n                  <\/jats:p>","DOI":"10.1111\/tra.12119","type":"journal-article","created":{"date-parts":[[2013,9,11]],"date-time":"2013-09-11T15:26:39Z","timestamp":1378913199000},"page":"1272-1289","source":"Crossref","is-referenced-by-count":337,"title":["Building a Better Dynasore: The Dyngo Compounds Potently Inhibit Dynamin and Endocytosis"],"prefix":"10.1111","volume":"14","author":[{"given":"Adam","family":"McCluskey","sequence":"first","affiliation":[{"name":"Chemistry, Centre for Chemical Biology, School of Environmental and Life Sciences The University of Newcastle Callaghan NSW 2308 Australia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"James A.","family":"Daniel","sequence":"additional","affiliation":[{"name":"Cell Signalling Unit Children's Medical Research Institute, 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