The bioactive Taxol conformation on β-tubulin:: Experimental evidence from highly active constrained analogs
The bioactive Taxol conformation on β-tubulin:: Experimental evidence from highly active constrained analogs
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DOI：
10.1073/pnas.0403459101
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发表时间：
2004-07-06
影响因子：
11.1
通讯作者：
Kingston, DGI
中科院分区：
文献类型：
--
作者：
Ganesh, T;Guza, RC;Kingston, DGI
重要的抗癌药物紫杉醇（紫杉醇）以化学计量比与微管蛋白结合，并促进其组装成微管。微管结合药物的构象一直是研究的主题，并提出了各种建议。在这项工作中，我们提出的实验和理论证据表明，紫杉醇采用T形构象时，它结合到微管蛋白。
The important anticancer drug Taxol (paclitaxel) binds to tubulin in a stoichiometric ratio and promotes its assembly into microtubules. The conformation of microtubule-bound drug has been the subject of intense study, and various suggestions have been made. In this work we present experimental and theoretical evidence that Taxol adopts a T-shaped conformation when it is bound to tubulin.