Pharmacokinetic characterization of CK2 inhibitor CX-4945

Archives of Pharmacal Research

Volumn 36, Issue 7, 2013, Pages 840-845

  Son, You Hwa ^a   Song, Jin Sook ^a   Kim, Seong Hwan ^a   Kim, Jiyeon ^a  

^a Korea Research Institute of Chemical Technology   (South Korea)

Author keywords

CK2; CX 4945; Druggability; Pharmacokinetics

Indexed keywords

CX 4945; CYTOCHROME P450; CYTOCHROME P450 1A; CYTOCHROME P450 2C19; CYTOCHROME P450 3A4; ENZYME INHIBITOR; PLASMA PROTEIN; POTASSIUM CHANNEL HERG; PROTEIN KINASE C; PROTEIN SERINE THREONINE KINASE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CELL MEMBRANE PERMEABILITY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG HALF LIFE; ENZYME INHIBITION; HUMAN; HUMAN CELL; LIVER MICROSOME; MALE; MDCK CELL; NONHUMAN; PROTEIN BINDING;

ANIMALS; CASEIN KINASE II; CELL MEMBRANE PERMEABILITY; DOGS; HEK293 CELLS; HUMANS; MADIN DARBY CANINE KIDNEY CELLS; MALE; MICROSOMES, LIVER; NAPHTHYRIDINES; RATS; RATS, SPRAGUE-DAWLEY;

EID: 84880044506     PISSN: 02536269     EISSN: 19763786     Source Type: Journal    
DOI: 10.1007/s12272-013-0103-9     Document Type: Article

References (35)

1. Battistutta, R., E. De Moliner, S. Sarno, G. Zanotti, and L.A. Pinna. 2001. Structural features underlying selective inhibition of protein kinase CK2 by ATP site-directed tetrabromo-2-benzotriazole. Protein Science 10: 2200-2206.
2. Belardinelli, L., C. Antzelevitch, and M.A. Vos. 2003. Assessing predictors of drug-induced torsade de pointes. Trends in Pharmacological Sciences 24: 619-625.
3. Buerra, B., and O.G. Issinger. 2008. Protein kinase CK2 in human diseases. Current Medicinal Chemistry 15: 1870-1886.
4. Drygin, D., C.B. Ho, M. Omori, J. Bliesath, C. Proffitt, R. Rice, A. Siddiqui-Jain, S. O'Brien, C. Padgett, J.K. Lim, K. Anderes, W.G. Rice, and D. Ryckman. 2011. Protein kinase CK2 modulates IL-6 expression in inflammatory breast cancer. Biochemical and Biophysical Research Communications 415: 163-167.
5. Duncan, J.S., and D.W. Litchfield. 2008. Too much of a good thing: the role of protein kinase CK2 in tumorigenesis and prospects for therapeutic inhibition of CK2. Biochimica et Biophysica Acta 1784: 33-47.
6. Hung, M.S., Z. Xu, Y.C. Lin, J.H. Mao, C.T. Yang, P.J. Chang, D.M. Jablons, and L. You. 2009. Identification of hematein as a novel inhibitor of protein kinase CK2 from a natural product library. BMC Cancer 9: 135.
7. Kim, J., and S.H. Kim. 2012. Druggability of the CK2 inhibitor CX-4945 as an anticancer drug and beyond. Archives of Pharmacal Research 35: 1293-1296.
8. Landesman-Bollag, E., R. Romieu-Mourez, D.H. Song, G.E. Sonenshein, R.D. Cardiff, and D.C. Seldin. 2001. Protein kinase CK2 in mammary gland tumorigenesis. Oncogene 20: 3247-3257.
9. Laramas, M., D. Pasquier, O. Filhol, F. Ringeisen, J.L. Descotes, and C. Cochet. 2007. Nuclear localization of protein kinase CK2 catalytic subunit (CK2alpha) is associated with poor prognostic factors in human prostate cancer. European Journal of Cancer 43: 928-934.
10. Litchfield, D.W. 2003. Protein kinase CK2: Structure, regulation and role in cellular decisions of life and death. Biochemical Journal 369: 1-15.
11. Ljubimov, A.V., S. Caballero, A.M. Aoki, L.A. Pinna, M.B. Grant, and R. Castellon. 2004. Involvement of protein kinase CK2 in angiogenesis and retinal neovascularization. Investigative Ophthalmology & Visual Science 45: 4583-4591.
12. Lopez-Ramos, M., R. Prudent, V. Moucadel, C.F. Sautel, C. Barette, L. Lafanechere, L. Mouaawad, D. Grierson, F. Schmidt, J.C. Florent, P. Filippakopoulos, A.N. Bullock, S. Knapp, J.B. Reiser, and C. Cochet. 2010. New potent dual inhibitors of CK2 and Pim kinases: Discovery and structural insights. FASEB Journal 24: 3171-3185.
13. Mottet, D., S.P. Ruys, C. Demazy, M. Raes, and C. Michiels. 2005. Role for casein kinase 2 in the regulation of HIF-1 activity. International Journal of Cancer 117: 764-774.
14. O-charoenrat, P., V. Rusch, and S.G. Talbot. 2004. Casein kinase II alpha subunit and C1-inhibitor are independent predictors of outcome in patients with squamous cell carcinoma of the lung. Clinical Cancer Research 10: 5792-5803.
15. Pagono, M.A., J. Bain, Z. Kazimierczuk, S. Sarno, M.Di. Ruzzene, G. Maira, M. Elliott, A. Orzeszko, G. Cozza, F. Meggio, and L.A. Pinna. 2008. The selectivity of inhibitors of protein kinase CK2: An update. Biochemical Journal 415: 353-365.
16. Parhar, J., J. Morse, and B. Salh. 2007. The role of protein kinase CK2 in intestinal epithelial cell inflammatory signaling. International Journal of Colorectal Disease 22: 601-609.
17. Park, J.S., M.S. Kim, J.S. Song, S.H. Choi, B.H. Lee, J. Woo, J.H. Ahn, M.A. Bae, and S.H. Ahn. 2011. Dose-independent pharmacokinetics of a new peroxisome proliferator-activated receptor-γ agonist, KR-62980, in Sprague-Dawley rats and ICR mice. Archives of Pharmacal Research 34: 2051-2058.
18. Pierre, F., P.C. Chua, S.E. O'Brien, A. Siddiqui-Jain, P. Bourbon, M. Haddach, J. Michaux, J. Nagasawa, M.K. Schwaebe, E. Stefan, A. Vialettes, J.P. Whitten, T.K. Chen, L. Darjania, R. Stansfield, K. Anderes, J. Bliesath, D. Drygin, C. Ho, M. Omori, C. Proffitt, N. Streiner, K. Trent, W.G. Rice, and D.M. Ryckman. 2011. Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]- naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. Journal of Medicinal Chemistry 5: 635-654.
19. Pistorius, K., G. Seitz, K. Remberger, and O.G. Issinger. 1991. Differential CKII activities in human colorectal mucosa, adenomas and carcinomas. Onkologie 14: 256-260.
20. Redfern, W.S., L. Carlsson, A.S. Davis, W.G. Lynch, I. Mackenzie, and S. Palethoroe. 2003. Relationship between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: Evidence for a provisional safety margin in drug development. Cardiovascular Research 58: 32-45.
21. Rendic, S., and F.J. Di Carlo. 1992. Human cytochrome P450 enzymes: A status report summarizing their reactions, substrates, inducers, and inhibitors. Drug Metabolism Reviews 29: 413-580.
22. Rodrigues, A.D. 1999. Integrated P450 reaction phenotyping: Attempting to bridge the gap between cDNA-expressed cytochromes P450 and native human liver microsomes. Biochemical Pharmacology 57: 465-480.
23. Ruiz-Garcia, A., M. Bermejo, A. Moss, and V.G. Casabo. 2008. Pharmacokinetics in drug discovery. Journal of Pharmaceutical Sciences 97: 654-690.
24. Ruzzene, M., and L.A. Pinna. 2010. Addition to protein kinase CK2: A common denominator of diverse cancer cells? Biochimica et Biophysica Acta 1804: 499-504.
25. Sandholt, I.S., B.B. Olsen, B. Guerra, and O.G. Issinger. 2009. Resorufin: A lead for a new protein kinase CK2 inhibitor. Anti-Cancer Drugs 20: 238-248.
26. Sarno, S., and L.A. Pinna. 2008. Protein kinase CK2 as a druggable target. Molecular BioSystems 4: 889-894.
27. Seldin, D.D., and P. Leder. 1995. Casein kinase II alpha transgene-induced murine lymphoma: Relation to theileriosis in cattle. Science 267: 894-897.
28. Siddiqui-Jain, A., D. Drygin, N. Streiner, P. Chua, F. Pierre, S.E. O'Brien, J. Blesath, M. Omori, N. Huser, C. Ho, C. Proffitt, M.K. Schwaebe, D.M. Ryckman, W.G. Rice, and K. Andres. 2010. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Research 70: 10288-10298.
29. Slaton, J.W., G.M. Unger, D.T. Sloper, A.T. Davis, and K. Ahmed. 2004. Introduction of apoptosis by antisense CK2 in human prostate cancer xenograft model. Molecular Cancer Research 2: 712-721.
30. Song, J.S., J.W. Chae, K.R. Lee, B.H. Lee, E.J. Choi, S.H. Ahn, K.I. Kwon, and M.A. Bae. 2011a. Pharmacokinetic characterization of decursinol derived from Angelica gigas Nakai in rats. Xenobiotica 41: 895-902.
31. Song, J.S., H.J. Rho, J.S. Park, M.S. Kim, B.H. Lee, J.W. Seo, D.J. Jeon, H.G. Cheon, S.H. Ahn, K.I. Kwon, and M.A. Bae. 2011b. Preclinical pharmacokinetics of PDE-310, a novel PDE4 inhibitor. Drug Metabolism and Pharmacokinetics 26: 192-200.
32. Stalter, G., S. Siemer, E. Becht, M. Ziegler, K. Remberger, and O.G. Issinger. 1994. Asymmetric expression of protein kinase CK2 subunits in human kidney tumors. Biochemical and Biophysical Research Communications 202: 141-147.
33. Thummel, K.E., and G. Wilkinson. 1998. In vitro and in vivo drug interactions involving human CYP3A. Annual Review of Pharmacology and Toxicology 38: 370-381.
34. van Golen, K.L., Z.F. Wu, X.T. Qiao, L. Bao, and S.D. Merajver. 2000. RhoC GTPase overexpression modulates induction of angiogenic factors in breast cells. Neoplasia 2: 418-425.
35. Wang, G., G. Unger, K.A. Ahmad, J.W. Slaton, and K. Ahmed. 2005. Downregulation of CK2 induces apoptosis in cancer cells - A potential approach to cancer therapy. Molecular and Cellular Biochemistry 274: 77-84.