Checkpoint kinase-1

Lyne PD, Kenny PW, Cosgrove DA, Deng C, Zabludoff S, Wendoloski JJ, Ashwell S. Identification of componnds with nanomolar binding affinity for checkpoint kinase-1 using knowledge-based virtual screening. J Med Chem 2004 47 1962-8. 

Van Holde KE, Zlatanova J, Arents G, Moudrianakis E (1995) Chromatin structure and gene expression (Elign SCR, ed). Oxford University Press, Oxford, ppl-26 Wang Y, Beerman TA, Kowalski D (2001) Antitumor drug adozelesin differentially affects active and silent origins of DNA replication in yeast checkpoint kinase mutants. Cancer Res 61(9) 3787-3794... 

Tse AN, Carvajal R, Schwartz GK. (2007) Targeting checkpoint kinase 1 in cancer therapeutics. Clin Cancer Res 13 1955-1960. 

Cole KA, Huggins J, Laquaglia M et al (2011) RNAi screen of the protein kinome identifies checkpoint kinase 1 (CHKl) as a therapeutic target in neuroblastoma. Proc Natl Acad Sci USA 108 3336-3341... 

Ganzinelli M, Carrassa L, Crippa F et al (2008) Checkpoint kinase 1 down-reguiation by an inducibie smaU interfering KNA expression system sensitized in vivo tumors to treatment with 5-fluorouracii. Ciin Cancer Res 14 5131-5141... 

Yu L, Graves P, Tempcyzk A, et al. The checkpoint kinase Chkl is a target of the anticancer agent UCN-01. Proc Am Assoc Cancer Res 1999 40 Abstract 2019. 

K., Register, J., Margosiak, S., Tempczyk-Russell, A., Nguyen, B., Myers, P., Lund-gren, ., Kan, . C., O Connor, P. M. (2000) The 1.7 A Crystal structure of human cell cycle checkpoint kinase Chkl implications for Chkl regulation. Cell 100, 681-692. 

Li, Q., Zhu, G.D. (2002) Targeting ser-ine/threonine protein kinase B/Akt and cell-cycle checkpoint kinases for treating cancer. Curr Top Med Chem.2, 939-971. 

Collins I, Garrett MD. 2005. Targeting the cell division cycle in cancer CDK and cell cycle checkpoint kinase inhibitors. Curr Opin Pharmacol 5 366-373. 

Isothiazoles have been incorporated into selective ChK2 (checkpoint kinase 2) inhibitor 212 <07BMCL172> and HCV (hepatitis C virus) NS5B polymerase inhibitor 213 <07BMCL28>, sultam into CDK (cyclin-dependent kinase) inhibitor 214 <07BMCL1284>, and trioxo-benzoisothiazole into the non-hepatotoxic acetaminophen analog 215 <07BMC2206>. 

As example of a checkpoint control, the response of the cell cycle in yeast to DNA damage will be described. Damaged DNA activates a checkpoint kinase (chkl) which is targeted to... 

B. Furnari, N. Rhind, and P. Russell. Cdc25 mitotic inducer targeted by chkl DNA damage checkpoint kinase [see comments]. Science, 277 (5331), 1495-1497, 1997. 

Chan GK, Jablonski SA, Sudakin V, Hittle JC, Yen TJ. Human BUBRl is a mitotic checkpoint kinase that monitors CENP-E functions at kinetochores and binds the cyclosome/APC. J. Cell. Biol. 1999 146 941-954. 

Syljuasen RG, Jensen S, Bartek J, Lukas J. Adaptation to the ionizing radiation-induced G2 checkpoint occurs in human cells and depends on checkpoint kinase 1 and Polo-like kinase 1 kinases. Cancer Res. 2006 66 10253-10257. 

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