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一种带有超长链间隔臂的生物素化紫杉醇的合成及生物学评价

Synthesis and Biological Evaluation of a Biotinylated Paclitaxel With an Extra-Long Chain Spacer Arm.

作者信息

Lis Lev G, Smart Mary A, Luchniak Anna, Gupta Mohan L, Gurvich Vadim J

机构信息

Institute for Therapeutics Discovery and Development and Department of Medicinal Chemistry, University of Minnesota, Minneapolis, Minnesota 55414, United States.

出版信息

ACS Med Chem Lett. 2012 Sep 13;3(9):745-748. doi: 10.1021/ml300149z. Epub 2012 Jul 30.

DOI:10.1021/ml300149z
PMID:23259031
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3523684/
Abstract

A biotinylated paclitaxel derivative with an extra-long-chain (LC-LC-Biotin) spacer arm was synthesized using an improved synthetic reaction sequence. The biotinylated paclitaxel analogue retained excellent microtubule stabilizing activity in vitro. Furthermore, it was shown that this analogue can simultaneously engage streptavidin and the binding site on microtubules, making it suitable for localization studies or for the attachment of paclitaxel to solid substrates via a streptavidin linkage.

摘要

使用改进的合成反应序列合成了一种带有超长链（LC-LC-生物素）间隔臂的生物素化紫杉醇衍生物。该生物素化紫杉醇类似物在体外保留了出色的微管稳定活性。此外，研究表明这种类似物能够同时与链霉亲和素和微管上的结合位点结合，使其适用于定位研究或通过链霉亲和素连接将紫杉醇附着于固体基质。

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本文引用的文献

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Taxanes: promising anti-cancer drugs.紫杉烷类：有前景的抗癌药物。
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Biotinylated PAMAM dendrimers for intracellular delivery of cisplatin to ovarian cancer: role of SMVT.生物素化 PAMAM 树枝状聚合物用于顺铂向卵巢癌细胞内的传递：SMVT 的作用。
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Synthesis and characterization of novel natural product-Gd(III) MRI contrast agent conjugates.新型天然产物-Gd(III)磁共振成像造影剂缀合物的合成与表征
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Development of Taxol and other endophyte produced anti-cancer agents.紫杉醇及其他内生菌产生的抗癌药物的研发。
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