A visible light-controllable Rho kinase inhibitor based on a photochromic phenylazothiazole
A visible light-controllable Rho kinase inhibitor based on a photochromic phenylazothiazole
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DOI：
10.1039/d1cc04905d
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发表时间：
2021-10-29
影响因子：
4.9
通讯作者：
Tamaoki, Nobuyuki
中科院分区：
文献类型：
--
作者：
Matsuo, Kazuya;Thayyil, Sampreeth;Tamaoki, Nobuyuki
Rho相关卷曲螺旋蛋白激酶（ROCK）是一种丝氨酸-苏氨酸激酶，其抑制剂可用于调节肌动球蛋白系统。在这里，我们开发了一种基于苯基偶氮噻唑支架的光开关ROCK抑制剂。通过可见光刺激的可逆的反-顺异构化使我们能够在体外和细胞中操纵ROCK活性。
Rho-associated coiled-coil-containing protein kinase (ROCK) is a serine-threonine kinase whose inhibitors are useful for the regulation of the actomyosin system. Here, we developed a photoswitchable ROCK inhibitor based on a phenylazothiazole scaffold. The reversible trans-cis isomerization by visible light stimuli enabled us to manipulate ROCK activities in vitro and in cells.