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Optical Control of CRAC Channels Using Photoswitchable Azopyrazoles.
Yang, Xingye; Ma, Guolin; Zheng, Sisi; Qin, Xiaojun; Li, Xiang; Du, Lupei; Wang, Youjun; Zhou, Yubin; Li, Minyong.
Afiliación
  • Yang X; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong 250012, China.
  • Ma G; Center for Translational Cancer Research, Institute of Biosciences and Technology, Texas A&M University, Houston, Texas 77030, United States.
  • Zheng S; Beijing Key Laboratory of Gene Resource and Molecular Development, College of Life Sciences, Beijing Normal University, Beijing 100875, China.
  • Qin X; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong 250012, China.
  • Li X; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong 250012, China.
  • Du L; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong 250012, China.
  • Wang Y; Beijing Key Laboratory of Gene Resource and Molecular Development, College of Life Sciences, Beijing Normal University, Beijing 100875, China.
  • Zhou Y; Center for Translational Cancer Research, Institute of Biosciences and Technology, Texas A&M University, Houston, Texas 77030, United States.
  • Li M; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, School of Pharmacy, Cheeloo College of Medicine, Shandong University, Jinan, Shandong 250012, China.
J Am Chem Soc ; 142(20): 9460-9470, 2020 05 20.
Article en En | MEDLINE | ID: mdl-32330031
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.

Texto completo: 1 Banco de datos: MEDLINE Idioma: En Revista: J Am Chem Soc Año: 2020 Tipo del documento: Article País de afiliación: China

Texto completo: 1 Banco de datos: MEDLINE Idioma: En Revista: J Am Chem Soc Año: 2020 Tipo del documento: Article País de afiliación: China