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• W2078769982 startingPage "1505" @default.
• W2078769982 abstract "Herein we demonstrate that competition between candidate kinetic stabilizer binding to transthyretin (TTR) and stilbene binding to and reaction with the same thyroxine sites within TTR can be utilized to discover potent and highly selective non-covalent TTR amyloidogenesis inhibitors. We report two stilbenes, S1 and S2, for use in distinct competition assays. Each bind selectively to TTR and then chemoselectively react to form an amide bond with the Lys-15 residue of TTR, creating a fluorescent conjugate. We used 28 TTR kinetic stabilizers exhibiting a known spectrum of plasma TTR binding selectivities and TTR amyloid fibril inhibition efficacies to validate the 'TTR fluorescence conjugate competition assay'. The kinetic stabilizers competed with S1 for binding to recombinant TTR in buffer and with S2 for binding to endogenous levels of TTR in human blood serum. In both assay scenarios, we demonstrate that the lower the TTR-stilbene conjugate fluorescence after a 3 h competition, the greater the binding selectivity and potency of the candidate TTR kinetic stabilizer. These assays, particularly the assay utilizing S2 in human serum, replace two assays previously utilized to gather the same information. While not the focus of this manuscript, it is clear that the 'TTR fluorescence conjugate competition assay' could be adapted for high throughput screening applications." @default.
• W2078769982 created "2016-06-24" @default.
• W2078769982 creator A5042980600 @default.
• W2078769982 creator A5081499831 @default.
• W2078769982 date "2011-02-01" @default.
• W2078769982 modified "2023-10-18" @default.
• W2078769982 title "A competition assay to identify amyloidogenesis inhibitors by monitoring the fluorescence emitted by the covalent attachment of a stilbene derivative to transthyretin" @default.
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• W2078769982 doi "https://doi.org/10.1016/j.bmc.2010.12.050" @default.
• W2078769982 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3039427" @default.
• W2078769982 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21273081" @default.
• W2078769982 hasPublicationYear "2011" @default.
• W2078769982 type Work @default.

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