Optical Control of CRAC Channels Using Photoswitchable Azopyrazoles.

J Am Chem Soc

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong 250012, China.

Published: May 2020

The Ca release-activated Ca (CRAC) channels control many Ca-modulated physiological processes in mammals. Hyperactivating CRAC channels are known to cause several human diseases, including Stormorken syndrome. Here, we show the design of azopyrazole-derived photoswitchable CRAC channel inhibitors (designated ), which enable optical inhibition of store-operated Ca influx and downstream signaling. Moreover, has been applied to alleviate thrombocytopenia and hemorrhage in a zebrafish model of Stormorken syndrome in a light-dependent manner.

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http://dx.doi.org/10.1021/jacs.0c02949DOI Listing

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