首页> 外文期刊>Combinatorial chemistry & high throughput screening >Chemogenomics and cancer chemotherapy: cell-based assays to screen for small molecules that impair microtubule dynamics.
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Chemogenomics and cancer chemotherapy: cell-based assays to screen for small molecules that impair microtubule dynamics.

机译:化学基因组学和癌症化学疗法:基于细胞的检测方法,筛选会损害微管动力学的小分子。

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摘要

Microtubules are still a promising target for new therapeutic agents. Thus, there is a continuous interest for compounds able to modify microtubule assembly, either by interacting directly with tubulin, or by interacting with microtubules regulators. Because of its dynamic characteristics, the microtubule cytoskeleton is a suitable target for small molecules that rapidly diffuse in the cell cytoplasm. Moreover, compounds targeting the microtubule cytoskeleton have proved to be valuable tools for basic research in cell biology. In this paper, after a short presentation of the apparent molecular pathways involved in the anticancer effect of agents that interfere with microtubules functions, the potentials and impact of chemogenomics and cell-based assays in the discovery of new therapeutic compounds and of new regulators of the microtubule cytoskeleton are described.
机译:微管仍然是新治疗剂的有希望的目标。因此,人们一直关注能够通过与微管蛋白直接相互作用或与微管调节剂相互作用来修饰微管组装的化合物。由于其动态特性,微管细胞骨架是快速扩散到细胞质中的小分子的合适靶标。而且,已证明靶向微管细胞骨架的化合物是细胞生物学基础研究的有价值的工具。在本文中,简要介绍了影响微管功能的药物的抗癌作用所涉及的明显分子途径,化学基因组学和基于细胞的测定在发现新的治疗化合物和新的调节剂中的潜力和影响。描述了微管细胞骨架。

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