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C-H Activation Generates Period-Shortening Molecules That Target Cryptochrome in the Mammalian Circadian Clock


Tsuyoshi Oshima, Iori Yamanaka, Anupriya Kumar, Junichiro Yamaguchi, Taeko Nishiwaki-Ohkawa, Kei Muto, Rika Kawamura, Tsuyoshi Hirota,  Kazuhiro Yagita,  Stephan Irle, Steve A. Kay, Takashi Yoshimura and Kenichiro Itami,

Angew. Chem., Int. Ed. 2015, Early View. DOI: 10.1002/anie.201502942

A change in rhythm: The first functional analysis of KL001 derivatives, which are mammalian circadian-clock modulators, was enabled by cutting-edge C[BOND]H activation. The sites of the KL001 derivatives that are critical for their rhythm-changing activity were elucidated, which led to the discovery of the first period-shortening molecules that target the cryptochrome.

 

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