作者:Xingye Yang、Guolin Ma、Sisi Zheng、Xiaojun Qin、Xiang Li、Lupei Du、Youjun Wang、Yubin Zhou、Minyong Li
DOI:10.1021/jacs.0c02949
日期:2020.5.20
The Ca2+ release-activated Ca2+ (CRAC) channels control many Ca2+-modulated physiological processes in mammals. Hyperactivating CRAC channels are known to cause Stormorken syndrome. Here we show the design of azopyrazole-derived photoswitchable CRAC channel inhibitors (designated piCRACs), which enable optical inhibition of store-operated Ca2+ influx and downstream signaling. Moreover, piCRAC-1 has
Ca2+ 释放激活的 Ca2+ (CRAC) 通道控制哺乳动物中许多 Ca2+ 调节的生理过程。众所周知,过度激活的 CRAC 通道会导致 Stormorken 综合征。在这里,我们展示了偶氮吡唑衍生的光开关 CRAC 通道抑制剂(指定为 piCRAC)的设计,它能够光学抑制存储操作的 Ca2+ 流入和下游信号传导。此外,piCRAC-1 已被应用于体内以光依赖的方式缓解 Stormorken 综合征斑马鱼模型中的血小板减少症和出血。