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Paclitaxel (PTX) is one of the most efficient anticancer drugs for the treatment of cancers through β-tubulin-binding. Our previous work indicated that a PTX-derivative hydroge-lator Fmoc-Phe-Phe-Lys(paclitaxel)-Tyr(H2PO3)-OH (1)could promote neuron branching but the underlying mechanism remains unclear. Using tubulin assembly-disassembly assay, in this work, we found that compound 1 obviously delayed more microtubule aggregation than PTX did. Under the catalysis of alkaline phosphatase, Fmoc-Phe-Phe-Lys(paclitaxel)-Tyr(H2PO3)-OH could self-assemble into nanofiber Fmoc-Phe-Phe-Lys(paclitaxel)-Tyr-OH with width comparable to the size of αβ-tubulin dimer. Therefore, we proposed in this work that nanofiber Fmoc-Phe-Phe-Lys(paclitaxel)-Tyr-OH not only inhibits the αβ-tubulin dimer binding to each other but also interferes with the plus end aggregation of microtubule. This work provides a new mechanism of the inhibition of microtubule formation by a PTX-derivative hydrogelator. 相似文献
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N-甲基为有机物分子中的一种常见基团.一九一五年Pregl首先应用Herzig-Meyer的常量法原理,建立N-甲基的微量定量分析法.反应原理与甲氧基的分析法同,但因N-甲基的化学键比甲氧基键稳定,N-甲基须先形成其季胺盐,然后再在较高温度分裂而得碘甲烷.生成的碘甲烷则同样象在甲氧基测定中以重量法或容量法测定之.N-甲基化合物与氢碘酸的反应因一次不能完成,故一般须经三、四次的重复蒸馏和热裂,方能获得较满意的结果. 相似文献
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