PF-4800567 explained

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]

Notes and References

  1. 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 . 26565986 . 6 . Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period . The Journal of Pharmacology and Experimental Therapeutics . 330 . 2 . 430–9 . August 2009 . 19458106 . 10.1124/jpet.109.151415 .
  2. 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 . 6 . Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes . Proceedings of the National Academy of Sciences of the United States of America . 107 . 34 . 15240–5 . August 2010 . 20696890 . 2930590 . 10.1073/pnas.1005101107 . 2010PNAS..10715240M . free .
  3. Perez DI, Gil C, Martinez A . Protein kinases CK1 and CK2 as new targets for neurodegenerative diseases . Medicinal Research Reviews . 31 . 6 . 924–54 . November 2011 . 20577972 . 10.1002/med.20207 . free . 10261/87060 . 206251000 .
  4. Etchegaray JP, Yu EA, Indic P, Dallmann R, Weaver DR . Casein kinase 1 delta (CK1delta) regulates period length of the mouse suprachiasmatic circadian clock in vitro . PLOS ONE . 5 . 4 . e10303 . April 2010 . 20421981 . 2858662 . 10.1371/journal.pone.0010303 . 2010PLoSO...510303E . Yamazaki S . free .
  5. Bryant CD, Graham ME, Distler MG, Munoz MB, Li D, Vezina P, Sokoloff G, Palmer AA . 6 . A role for casein kinase 1 epsilon in the locomotor stimulant response to methamphetamine . Psychopharmacology . 203 . 4 . 703–11 . May 2009 . 19050854 . 2729782 . 10.1007/s00213-008-1417-z .
  6. Bryant CD, Parker CC, Zhou L, Olker C, Chandrasekaran RY, Wager TT, Bolivar VJ, Loudon AS, Vitaterna MH, Turek FW, Palmer AA . 6 . Csnk1e is a genetic regulator of sensitivity to psychostimulants and opioids . Neuropsychopharmacology . 37 . 4 . 1026–35 . March 2012 . 22089318 . 3280656 . 10.1038/npp.2011.287 .

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