(-)-Blebbistatin

(-)-Blebbistatin是一种细胞通透性的非肌肉肌球蛋白II型ATP酶抑制剂，IC50值为2 μM [1,2]。

非肌肉肌球蛋白II（NM II），肌动蛋白结合蛋白，在调节细胞迁移、粘附和分化中起重要作用 [4]。NM II在这些过程中的重要性通过基因缺失和突变的方法进行研究，发现NM II突变影响范围广泛的蛋白功能，引起单基因遗传病 [5,6]。

(-)-Blebbistatin是一种小分子抑制剂，优先结合肌球蛋白-ADP-Pi复合体，从而减慢磷酸根的释放 [2]。在几个物种的体外实验中，(-)-Blebbistatin完全消除肌动蛋白激活的Mg-ATPase收缩活性和肌球蛋白II的收缩动力（IC50 = 0.5-5.0 μM）[8,9]，但对平滑肌肌球蛋白II（IC50 =80 μM），和肌球蛋白I、V和X的影响很小 [3]。而且，blebbistatin可以抑制哺乳动物动脉平滑肌（IC50=5 μM）[9]。Blebbistatin阻断肌动蛋白分离状态下的肌球蛋白II和防止僵化肌动球蛋白交联的特性是其体内应用的一个很大的优势 [2,11]。

在恒压灌注模型系统中，CB和TM细胞用blebbistatin（10-200 M）处理后，细胞形态发生改变，肌动蛋白应力纤维的含量降低。Blebbistatin的效应在24小时内洗脱后是完全可逆的 [10]。Blebbistatin抑制单个细胞的收缩，而不改变细胞内钙瞬变（IC50 = 0.43 μM）的形态。

参考文献：
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