Effects of the hydrophobicity of taxoids on their interaction with tubulin.
Effects of the hydrophobicity of taxoids on their interaction with tubulin.
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DOI：
10.1016/s0968-0896(99)00279-5
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发表时间：
2000
影响因子：
3.5
通讯作者：
D. Guénard;S. Thoret;J. Dubois;M. Adeline;Q. Wang;F. Gueritte
中科院分区：
文献类型：
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作者：
D. Guénard;S. Thoret;J. Dubois;M. Adeline;Q. Wang;F. Gueritte
类taxoids在7和10位置的疏水特性的修饰极大地改变了这些药物对微管-微管系统的作用。烷基链的存在降低了这些分子的活性，而相应的极性更强的类似物则恢复了这些分子的活性。微管蛋白对类taxoids的识别似乎取决于最重要疏水区域的位置。
Modifications of the hydrophobic character at the 7 and 10 positions of the taxoids greatly modified the effect of these drugs on the tubulin–microtubule system. The presence of an alkyl chain at these positions decreased the activity while their corresponding more polar analogues restored the activity of these molecules. It appears that the recognition of taxoids by tubulin depends on the location of the most important hydrophobic area.