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首页> 外文期刊>Nanotechnology >Comparative modelling of human beta tubulin isotypes and implications for drag binding
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Comparative modelling of human beta tubulin isotypes and implications for drag binding

机译：人β微管蛋白同种型的比较建模及其对药物结合的影响

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摘要

The protein tubulin is a target for several anti-mitotic drugs, which affect microtubule dynamics, ultimately leading to cell cycle arrest and apoptosis. Many of these drugs, including the taxanes and Vinca alkaloids, are currently used clinically in the treatment of several types of cancer. Another tubulin binding drug, colchicine, although too toxic to be used as a chemotherapeutic agent, is commonly used for the treatment of gout. The main disadvantage that all of these drugs share is that they bind tubulin indiscriminately, leading to the death of both cancerous and healthy cells. However, the broad cellular distribution of several tubulin isotypes provides a platform upon which to construct novel chemotherapeutic drugs that could differentiate between different cell types, reducing the undesirable side effects associated with current chemotherapeutic treatments. Here, we report an analysis of ten human beta tubulin isotypes and discuss differences within each of the previously characterized paclitaxel, colchicine and vinblastine binding sites.
机译：蛋白微管蛋白是几种抗有丝分裂药物的靶标，这些药物影响微管动力学，最终导致细胞周期停滞和凋亡。这些药物中的许多，包括紫杉烷类和长春花生物碱，目前在临床上用于治疗几种类型的癌症。另一种微管蛋白结合药物秋水仙碱，尽管毒性太大而不能用作化学治疗剂，但通常用于治疗痛风。所有这些药物共有的主要缺点是它们不加选择地结合微管蛋白，导致癌细胞和健康细胞死亡。然而，几种微管蛋白同种型的广泛细胞分布提供了构建新的化学治疗药物的平台，该新的化学治疗药物可以区分不同的细胞类型，从而减少了与当前化学治疗相关的不良副作用。在这里，我们报告了对十种人类β微管蛋白同种型的分析，并讨论了每个先前表征的紫杉醇，秋水仙碱和长春碱结合位点之间的差异。

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