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Long chain amines and long chain ammonium salts as novel inhibitors of dynamin GTPase activity.
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2004 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1090-2120, Vol. 14, no 12Article in journal (Refereed) Published
Abstract [en]

We examined a number of ligands with the view of inhibiting the GTPase activity of dynamin. Dynamin contains a pleckstrin homology (PH) domain that interacts with lipids. We report a series of simple lipid-like molecules that display moderate inhibitory activity. Inhibitory activity is linked to chain length and quaternarization of the terminal amine. A change in the counterion, Cl versus Br or I, had little effect on potency. However, introduction of a hydrophobic collar proximal to the charged site was beneficial to dynamin GTPase inhibitory action. The most potent compound was myristoyl trimethyl ammonium bromide (MTMAB, IC(50) 3.15 microM).

Place, publisher, year, edition, pages
2004. Vol. 14, no 12
National Category
Organic Chemistry
URN: urn:nbn:se:uu:diva-272674DOI: 10.1016/j.bmcl.2004.03.096PubMedID: 15149689OAI: oai:DiVA.org:uu-272674DiVA: diva2:894581
Available from: 2016-01-15 Created: 2016-01-15 Last updated: 2016-01-15

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Odell, Luke R
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