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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).

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2004. Vol. 14, no 12
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Organic Chemistry
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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: 2017-11-30

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Odell, Luke R

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