Cited by 194Circadian rhythm and melatoninSleep and Work-Related FatigueSleep and Wakefulness Research

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Selective Inhibition of Casein Kinase 1ϵ Minimally Alters Circadian Clock Period

Walton, Kevin M., Fisher, Katherine, Rubitski, David, Marconi, Michael, Meng, Qing-Jun, Sládek, Martin, Adams, Jessica, Bass, Michael, Chandrasekaran, Rama, Butler, Todd, Griffor, Matt, Rajamohan, Francis, Serpa, Megan, Chen, Yuhpyng, Claffey, Michelle, Hastings, Michael, Loudon, Andrew, Maywood, Elizabeth, Ohren, Jeffrey, Doran, Angela, Wager, Travis T.·2009·The Journal of Pharmacology and Experimental Therapeutics

DOI 10.1124/jpet.109.151415

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Abstract

The circadian clock links our daily cycles of sleep and activity to the external environment. Deregulation of the clock is implicated in a number of human disorders, including depression, seasonal affective disorder, and metabolic disorders. Casein kinase 1 epsilon (CK1epsilon) and casein kinase 1 delta (CK1delta) are closely related Ser-Thr protein kinases that serve as key clock regulators as demonstrated by mammalian mutations in each that dramatically alter the circadian period. Therefore, inhibitors of CK1delta/epsilon may have utility in treating circadian disorders. Although we previously demonstrated that a pan-CK1delta/epsilon inhibitor, 4-[3-cyclohexyl-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyrimidin-2-ylamine (PF-670462), causes a significant phase delay in animal models of circadian rhythm, it remains unclear whether one of the kinases has a predominant role in regulating the circadian clock. To test this, we have characterized 3-(3-chloro-phenoxymethyl)-1-(tetrahydro-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine (PF-4800567), a novel and potent inhibitor of CK1epsilon (IC(50) = 32 nM) with greater than 20-fold selectivity over CK1delta. PF-4800567 completely blocks CK1epsilon-mediated PER3 nuclear localization and PER2 degradation. In cycling Rat1 fibroblasts and a mouse model of circadian rhythm, however, PF-4800567 has only a minimal effect on the circadian clock at concentrations substantially over its CK1epsilon IC(50). This is in contrast to the pan-CK1delta/epsilon inhibitor PF-670462 that robustly alters the circadian clock under similar conditions. These data indicate that CK1epsilon is not the predominant mediator of circadian timing relative to CK1delta. PF-4800567 should prove useful in probing unique roles between these two kinases in multiple signaling pathways.

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Authors: Walton, K. M., Fisher, K., Rubitski, D., Marconi, M., Meng, Q.-J., Sládek, M., Adams, J., Bass, M., Chandrasekaran, R., Butler, T., Griffor, M., Rajamohan, F., Serpa, M., Chen, Y., Claffey, M., Hastings, M., Loudon, A., Maywood, E., Ohren, J., Doran, A., & Wager, T. T.
Affiliations: Pfizer (United States) (US)
ORCID: Fisher, Katherine
Meng, Qing-Jun
Sládek, Martin
Bass, Michael
Hastings, Michael
Loudon, Andrew
Maywood, Elizabeth
Ohren, Jeffrey
Doran, Angela
Wager, Travis T.
Venue: The Journal of Pharmacology and Experimental Therapeutics
Publisher: Elsevier BV
Published: 2009-08
Volume: 330
Issue: 2
Pages: 430-439
ISSN: 0022-3565 (ISSN-L)
DOI: 10.1124/jpet.109.151415
OpenAlex: W2114428498
Cited by: 184
References: 34
Citations by year: 2026: 13 · 2025: 10 · 2024: 9 · 2023: 2 · 2022: 7 · 2021: 9 · 2020: 11 · 2019: 17 · 2018: 10 · 2017: 12 · 2016: 7 · 2015: 13 · 2014: 13 · 2013: 11 · 2012: 12
FWCI: 5.98
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Journal of Pharmacology and Experimental Therapeutics (publishedVersion)
PubMed (publishedVersion)
Research Explorer (The University of Manchester) (publishedVersion)
Funders: Biotechnology and Biological Sciences Research Council (BB/E022553/1)
Topics: Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Circadian rhythm and melatonin
Social Sciences › Psychology › Experimental and Cognitive Psychology › Sleep and Work-Related Fatigue
Life Sciences › Neuroscience › Cognitive Neuroscience › Sleep and Wakefulness Research
Keywords: CK1ε, CK1δ, circadian clock, circadian period, kinase inhibitors, circadian rhythm, circadian disorders, selective kinase inhibition
MeSH terms: Animals, Circadian Rhythm, Dose-Response Relationship, Drug, Humans, Male, Mice, Inbred C57BL, Pyrazoles, Pyrimidines, Protein Kinase Inhibitors, Casein Kinase 1 epsilon, Mice

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Selective Inhibition of Casein Kinase 1ϵ Minimally Alters Circadian Clock Period

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