小分子抗肿瘤蛋白激酶抑制剂的研究进展

史宁 韦林毅 吴久鸿

中国药学杂志 ›› 2011, Vol. 46 ›› Issue (23) : 1784-1789.

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中国药学杂志 ›› 2011, Vol. 46 ›› Issue (23) : 1784-1789.
综述

小分子抗肿瘤蛋白激酶抑制剂的研究进展

  • 史宁,韦林毅,吴久鸿*
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摘要

目的 综述小分子抗肿瘤蛋白激酶抑制剂的研究进展。方法 以近5年文献为主要依据,对激酶靶点及小分子抑制剂的研究发展变化进行分析、整理和总结。结果 呈现由单作用靶点抑制剂向多作用靶点抑制剂、由单一选择性抑制剂向多选择性抑制剂发展的变化趋势,由于蛋白激酶的结构突变,第一代抑制剂陆续出现耐药,导致众多作用于结构突变位点的新型抑制剂的出现。结论 随着结构生物学和计算机辅助药物分子设计技术的进步,基于药物合理设计的小分子激酶抑制剂会有更广阔的发展前景。

关键词

激酶抑制剂 / 蛋白酪氨酸激酶 / 抗肿瘤药物 / 多靶点抑制剂 / 耐药蛋白激酶

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史宁 韦林毅 吴久鸿. 小分子抗肿瘤蛋白激酶抑制剂的研究进展[J]. 中国药学杂志, 2011, 46(23): 1784-1789

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