کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1936852 | 1050703 | 2007 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Potent inhibition of tau fibrillization with a multivalent ligand
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کلمات کلیدی
HEPESODS4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid - 4- (2-hydroxyethyl) -1-piperazineethanesulfonic acidDMSO - DMSOAlzheimer’s disease - بیماری آلزایمرAggregation - تجمعNeurofibrillary tangle - خلط نوروفیبریلاTau - خود راDimethyl sulfoxide - دیمتیل سولفواکسیدCyanine dye - رنگ سیانینMass spectroscopy - طیف سنجی جرمیliquid chromatography - کروماتوگرافی مایع
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
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چکیده انگلیسی
Small-molecule inhibitors of tau fibrillization are under investigation as tools for interrogating the tau aggregation pathway and as potential therapeutic agents for Alzheimer's disease. Established inhibitors include thiacarbocyanine dyes, which can inhibit recombinant tau fibrillization in the presence of anionic surfactant aggregation inducers. In an effort to increase inhibitory potency, a cyclic bis-thiacarbocyanine molecule containing two thiacarbocyanine moieties was synthesized and characterized with respect to tau fibrillization inhibitory activity by electron microscopy and ligand aggregation state by absorbance spectroscopy. Results showed that the inhibitory activity of the bis-thiacarbocyanine was qualitatively similar to a monomeric cyanine dye, but was more potent with 50% inhibition achieved at â¼80Â nM concentration. At all concentrations tested in aqueous solution, the bis-thiacarbocyanine collapsed to form a closed clamshell structure. However, the presence of tau protein selectively stabilized the open conformation. These results suggest that the inhibitory activity of bis-thiacarbocyanine results from multivalency, and reveal a route to more potent tau aggregation inhibitors.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical and Biophysical Research Communications - Volume 363, Issue 1, 9 November 2007, Pages 229-234
Journal: Biochemical and Biophysical Research Communications - Volume 363, Issue 1, 9 November 2007, Pages 229-234
نویسندگان
Nicolette S. Honson, Jordan R. Jensen, Michael V. Darby, Jeff Kuret,