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Aza-BODIPY:改进的合成方法及与可溶性 Aβ1-42 寡聚物的相互作用。

Aza-BODIPY: improved synthesis and interaction with soluble Aβ1-42 oligomers.

机构信息

Department of Chemistry, Texas Christian University, Fort Worth, TX 76129, USA.

出版信息

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1732-5. doi: 10.1016/j.bmcl.2013.01.065. Epub 2013 Jan 31.

Abstract

Dye-binding assays that are used to evaluate anti-aggregation ability of small molecule inhibitors towards amyloids are known to be prone to false-positive effects due to spectral overlaps between the dye and the inhibitor. Aza-BODIPY dye, which has both excitation and emission maxima above 600nm, exhibits a significant increase in its fluorescence intensity in the presence of soluble oligomers of Aβ1-42. These results indicate that aza-BODIPY could serve as a near-IR probe for detecting conformational changes of Aβ1-42 soluble oligomers in vitro, and it should eliminate false-positive effects that are associated with currently utilized thioflavin T-based dyes. In addition, a facile synthesis of aza-BODIPY has been developed, which might further expand the applications of this dye.

摘要

用于评估小分子抑制剂对淀粉样蛋白聚集能力的染料结合测定法由于染料和抑制剂之间的光谱重叠,容易产生假阳性效应。吖啶-BODIPY 染料的激发和发射最大值均高于 600nm,在存在 Aβ1-42 的可溶性寡聚物的情况下,其荧光强度显著增加。这些结果表明,吖啶-BODIPY 可以作为近红外探针,用于检测 Aβ1-42 可溶性寡聚物的构象变化,并且应该消除与目前使用的硫代黄素 T 基染料相关的假阳性效应。此外,已经开发出吖啶-BODIPY 的简便合成方法,这可能进一步扩展该染料的应用。

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