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- Title
CH Activation Generates Period-Shortening Molecules That Target Cryptochrome in the Mammalian Circadian Clock.
- Authors
Oshima, Tsuyoshi; Yamanaka, Iori; Kumar, Anupriya; Yamaguchi, Junichiro; Nishiwaki-Ohkawa, Taeko; Muto, Kei; Kawamura, Rika; Hirota, Tsuyoshi; Yagita, Kazuhiro; Irle, Stephan; Kay, Steve A.; Yoshimura, Takashi; Itami, Kenichiro
- Abstract
The synthesis and functional analysis of KL001 derivatives, which are modulators of the mammalian circadian clock, are described. By using cutting-edge CH activation chemistry, a focused library of KL001 derivatives was rapidly constructed, which enabled the identification of the critical sites on KL001 derivatives that induce a rhythm-changing activity along with the components that trigger opposite modes of action. The first period-shortening molecules that target the cryptochrome (CRY) were thus discovered. Detailed studies on the effects of these compounds on CRY stability implicate the existence of an as yet undiscovered regulatory mechanism.
- Subjects
CARBON-hydrogen bonds; CHEMICAL synthesis; CIRCADIAN rhythms; CRYPTOCHROMES; STRUCTURE-activity relationships; MAMMALS
- Publication
Angewandte Chemie, 2015, Vol 127, Issue 24, p7299
- ISSN
0044-8249
- Publication type
Article
- DOI
10.1002/ange.201502942