一种简化的荧光标记 discodermolide 的设计、合成及生物评价，作为研究 discodermolide 与微管蛋白结合的分子探针。
Design, synthesis and biological evaluation of a simplified fluorescently labeled discodermolide as a molecular probe to study the binding of discodermolide to tubulin.
机构信息
Department of Chemistry, Virginia Tech, Blacksburg, VA 24061, USA.
出版信息
Bioorg Med Chem. 2011 Sep 1;19(17):5247-54. doi: 10.1016/j.bmc.2011.06.082. Epub 2011 Jul 2.
Abstract
The design, synthesis, and biological evaluation of a simplified fluorescently labeled discodermolide analogue possessing a dimethylaminobenzoyl fluorophore has been achieved. Stereoselective Suzuki coupling and Horner-Wadsworth-Emmons reaction comprised the key tactics for its construction. The analogue exhibited qualitatively similar activity to paclitaxel in a tubulin assembly assay, and it can thus be used as a fluorescent molecular probe to explore the local environment of the discodermolide binding site on tubulin. The results of fluorescence measurements on the tubulin-bound analogue are reported.
摘要
已经实现了一种简化的荧光标记 discodermolide 类似物的设计、合成和生物评价，该类似物具有二甲氨基苯甲酰荧光团。立体选择性的 Suzuki 偶联和 Horner-Wadsworth-Emmons 反应是其构建的关键策略。该类似物在微管蛋白组装测定中表现出与紫杉醇定性相似的活性，因此可以用作荧光分子探针来探索 discodermolide 结合部位在微管蛋白上的局部环境。报告了结合在微管蛋白上的类似物的荧光测量结果。
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