The structural basis of blebbistatin inhibition and specificity for myosin II
The structural basis of blebbistatin inhibition and specificity for myosin II
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DOI：
10.1038/nsmb908
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发表时间：
2005-04-01
影响因子：
16.8
通讯作者：
Rayment, I
中科院分区：
文献类型：
--
作者：
Allingham, JS;Smith, R;Rayment, I
分子马达在细胞内介导的细胞过程中起着核心作用，因此是药理学药物控制细胞的一个很好的靶点。然而，很少有这样的化合物已被发现。我们在这里报告的结构blebbistatin，抑制特定的肌球蛋白亚型，绑定到电机域的Dictyosteelium discoideum肌球蛋白II。这揭示了其特异性的结构基础，并为新药物的开发提供了见解。
Molecular motors play a central role in cytoskeletal-mediated cellular processes and thus present an excellent target for cellular control by pharmacological agents. Yet very few such compounds have been found. We report here the structure of blebbistatin, which inhibits specific myosin isoforms, bound to the motor domain of Dictyostelium discoideum myosin II. This reveals the structural basis for its specificity and provides insight into the development of new agents.