PF-4800567
PF-4800567 is a drug developed by Pfizer which acts as a selective inhibitor of the enzyme 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,[1][2] as well as showing potential neuroprotective effects.[3] While this research has shown that circadian rhythm is modulated primarily by the alternate isoform CK1-δ rather than CK1-ε,[4] 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.[5][6]
References[edit | edit source]
- ↑ 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
- ↑ 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
- ↑
- ↑
- ↑ 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
- ↑ PMID 22089318
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