Ontology highlight
ABSTRACT:
SUBMITTER: Lee JW
PROVIDER: S-EPMC8901179 | biostudies-literature | 2019 Feb
REPOSITORIES: biostudies-literature
Lee Jae Wook JW Hirota Tsuyoshi T Ono Daisuke D Honma Sato S Honma Ken-Ichi KI Park Keunwan K Kay Steve A SA
Journal of medicinal chemistry 20190215 4
Circadian rhythms are controlled by transcriptional feedback loops of clock genes and proteins. The stability of clock proteins is regulated by post-translational modification, such as phosphorylation by kinases. In particular, casein kinase I (CKI) phosphorylates the PER protein to regulate proteasomal degradation and nuclear localization. Therefore, CKI inhibition can modulate mammalian circadian rhythms. In the present study, we have developed novel CKIα and CKIδ dual inhibitors by extensive ...[more]