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[微管聚合抑制剂——新型天然化合物作为潜在抗癌药物]

[Inhibitors of microtubule polymerization- new natural compounds as potential anti-cancer drugs].

作者信息

Rogalska Aneta, Miśkiewicz Klaudia, Marczak Agnieszka

机构信息

Katedra Termobiologii, Instytut Biofizyki, Wydział Biologii i Ochrony Środowiska, Uniwersytet Łódzki.

出版信息

Postepy Hig Med Dosw (Online). 2015 May 4;69:571-85. doi: 10.5604/17322693.1151293.

Abstract

Inhibitors of microtubule polymerization are compounds which, by binding to the tubulin dimer, prevent the normal course of cell division and lead to cell death. They cause inhibition of mitosis, affect the cytoskeleton and disrupt the process of angiogenesis. Inhibitors of microtubule polymerization include natural substances, synthetic and semi-synthetic analogs. They contain a group of compounds having the ability to bind to the vinca alkaloid and colchicine domain of β-tubulin. Among them are vinca alkaloids, dolastatins and halichondrins, which connect to the vinca alkaloids domain, and combretastatins binding the colchicine site of protein. Tumor cells have greater capacity for cell proliferation and are also more susceptible to damage by microtubule inhibitors. Their action has been widely used in cancer therapy.

摘要

微管聚合抑制剂是一类通过与微管蛋白二聚体结合,阻止细胞正常分裂进程并导致细胞死亡的化合物。它们会抑制有丝分裂,影响细胞骨架并破坏血管生成过程。微管聚合抑制剂包括天然物质、合成及半合成类似物。它们含有一组能够与β-微管蛋白的长春花生物碱和秋水仙碱结构域结合的化合物。其中有与长春花生物碱结构域相连的长春花生物碱、多拉司他汀和海兔毒素,以及结合蛋白质秋水仙碱位点的康普瑞他汀。肿瘤细胞具有更强的细胞增殖能力,也更容易受到微管抑制剂的损伤。它们的作用已广泛应用于癌症治疗。

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