Recent advances in the structure-based rational design of TNKSIs.
Recent advances in the structure-based rational design of TNKSIs.
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DOI：
10.1039/c4mb00385c
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发表时间：
2014-09
影响因子：
--
通讯作者：
P. Zhan;Yu'ning Song;Yukihiro Itoh;Takayoshi Suzuki;Xinyong Liu
中科院分区：
文献类型：
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作者：
P. Zhan;Yu'ning Song;Yukihiro Itoh;Takayoshi Suzuki;Xinyong Liu
人端锚聚合酶1和2（TNKS 1/2）是有吸引力的药理学生物靶标，特别是用于治疗特定类型的癌症。本文提供了一个相当全面的概述TNKS-抑制剂复合物的结构生物学和目前的药物化学策略中使用的基于结构的合理设计的端锚聚合酶特异性抑制剂。
Human tankyrases 1 and 2 (TNKS1/2) are attractive pharmacological biotargets, especially for the treatment of specific types of cancer. This article provides a fairly comprehensive overview of the structural biology of the TNKS-inhibitor complex and the current medicinal chemistry strategies being used in the structure-based rational design of tankyrase-specific inhibitors.