新型致癌蛋白激酶抑制剂用于癌症治疗。

Tomi K Sawyer
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引用次数: 34

摘要

癌症治疗的小分子药物发现在推进新型致癌蛋白激酶抑制剂先导化合物领域取得了非凡的进展,对基础研究和临床试验都有重大影响。从这个角度来看,基于结构和机制的药物设计相对于这些进展是突出的。此外,与治疗靶标选择性相关的新型致癌蛋白激酶抑制剂药物发现的不断发展的概念也得到了强调,包括最近发现的影响耐药或增强对小分子抑制剂药物敏感性的致癌激酶突变体。
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Novel oncogenic protein kinase inhibitors for cancer therapy.

Small-molecule drug discovery for cancer therapy is making extraordinary progress within the realm of advancing novel oncogenic protein kinase inhibitor lead compounds of significant impact to both basic research and clinical testing. In this perspective, structure- and mechanism-based drug design are highlighted relative to such progress. Also, evolving concepts in novel oncogenic protein kinase inhibitor drug discovery is highlighted relative to therapeutic target selectivity, including the recent identification of oncogenic kinase mutants effecting drug-resistance or enhanced drug susceptibility to small-molecule inhibitors.

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