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A methylbenzimidazole derivative regulates mammalian circadian rhythms by targeting Cryptochrome proteins.


ABSTRACT: Background: Impairment of the circadian clock has been associated with numerous diseases, including sleep disorders and metabolic disease. Although small molecules that modulate clock function may form the basis of drug discovery of clock-related diseases, only a few compounds that selectively target core clock proteins have been identified. Three scaffolds were previously discovered as small-molecule activators of the clock protein Cryptochrome (CRY), and they have been providing powerful tools to understand and control the circadian clock system. Identifying new scaffolds will expand the possibilities of drug discovery. Methods: A methylbenzimidazole derivative TH401 identified from cell-based circadian screens was characterized. Effects of TH401 on circadian rhythms were e

SUBMITTER: Yagi M 

PROVIDER: S-EPMC9523283 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature