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Progress in the design of selective ATP-competitive kinase inhibitors
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 12
- DOI:
- 10.3321/j.issn:0513-4870.2007.12.002
- Key Word:
- 蛋白激酶抑制剂;特异性;ATP竞争性;药物设计
Abstract： 激酶在细胞的生命过程中起着至关重要的作用,其功能异常会导致包括肿瘤在内的许多重大疾病的发生.针对疾病相关的激酶靶标,研发ATP竞争性的小分子激酶抑制剂成为当前的热点.但激酶催化域的结构和序列高度保守,使得许多激酶抑制剂的选择性都比较低.近年来,随着结构生物学和计算机辅助药物分子设计技术的进步,选择性的ATP竞争性激酶抑制剂的研发取得了很大的进展,本文拟就近年来选择性的激酶抑制剂设计研究进展作一综述.
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