Prab at 12:06, 26 September 2023

2023-09-26T12:06:03Z

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[[File:PF-4800567_structure.png|thumb|{{PAGENAME}} structure]]

'''PF-4800567''' is a drug developed by [[Pfizer]] which acts as a selective inhibitor of the [[enzyme]] [[CSNK1E|Casein kinase 1 epsilon]] (CK1-ε), and has mainly been used in the study of the casein kinase 1 enzymes in the regulation of [[circadian rhythm]],<ref>Walton KM, Fisher K, Rubitski D, Marconi M, Meng QJ, 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 TT. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. ''Journal of Pharmacology and Experimental Therapeutics''. 2009 Aug;330(2):430-9. PMID 19458106</ref><ref>Meng QJ, Maywood ES, Bechtold DA, Lu WQ, Li J, Gibbs JE, Dupré SM, Chesham JE, Rajamohan F, Knafels J, Sneed B, Zawadzke LE, Ohren JF, Walton KM, Wager TT, Hastings MH, Loudon AS. Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. ''Proceedings of the National Academy of Sciences USA''. 2010 Aug 24;107(34):15240-5. PMID 20696890</ref> as well as showing potential [[neuroprotective]] effects.<ref>{{Cite doi|10.1002/med.20207}}</ref> While this research has shown that circadian rhythm is modulated primarily by the alternate isoform CK1-δ rather than CK1-ε,<ref>{{Cite doi|10.1371/journal.pone.0010303}}</ref> both PF-4800567 and the related non-selective CK1-δ/ε inhibitor PF-670462 were found in animal studies to enhance responses to certain drugs of abuse such as [[methamphetamine]] and [[fentanyl]], which suggests a role for CK1-ε in negative regulation of sensitivity to [[stimulant]] and [[opioid]] drugs.<ref>Bryant CD, Graham ME, Distler MG, Munoz MB, Li D, Vezina P, Sokoloff G, Palmer AA. A role for casein kinase 1 epsilon in the locomotor stimulant response to methamphetamine. ''Psychopharmacology (Berlin)''. 2009 May;203(4):703-11. PMID 19050854</ref><ref>{{Cite doi|10.1038/npp.2011.287}} PMID 22089318</ref>

== References ==
{{Reflist}}

{{pharm-stub}}

[[Category:Enzyme inhibitors]]
[[Category:Pfizer]]

PF-4800567 - Revision history

Prab at 12:06, 26 September 2023