Optical Control of CRAC Channels Using Photoswitchable Azopyrazoles.

abstract

• The Ca2+ release-activated Ca2+ (CRAC) channels control many Ca2+-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 piCRACs), which enable optical inhibition of store-operated Ca2+ influx and downstream signaling. Moreover, piCRAC-1 has been applied in vivo to alleviate thrombocytopenia and hemorrhage in a zebrafish model of Stormorken syndrome in a light-dependent manner.

altmetric score

• 3.5

author list (cited authors)

• Yang, X., Ma, G., Zheng, S., Qin, X., Li, X., Du, L., ... Li, M.

citation count

• 21

complete list of authors

• Yang, Xingye||Ma, Guolin||Zheng, Sisi||Qin, Xiaojun||Li, Xiang||Du, Lupei||Wang, Youjun||Zhou, Yubin||Li, Minyong

publisher

• American Chemical Society (ACS)  Publisher

published in

• Journal of the American Chemical Society  Journal

keywords

• 1 Underpinning Research
• 1.1 Normal Biological Development And Functioning

PubMed Central ID

• 32330031

Digital Object Identifier (DOI)

• 10.1021/jacs.0c02949

start page

• 9460

end page

• 9470

volume

• 142

issue

• 20

URL

• http://dx.doi.org/10.1021/jacs.0c02949