Development and exploitation of CK2 inhibitors

Molecular and Cellular Biochemistry

Volumn 274, Issue 1-2, 2005, Pages 69-76

  Sarno, Stefania ^a   Ruzzene, Maria ^a   Frascella, Pietrogiulio ^b   Pagano, Mario A ^a   Meggio, Flavio ^a   Zambon, Alfonso ^b   Mazzorana, Marco ^a   Di Maira, Giovanni ^a   Lucchini, Vittorio ^b   Pinna, Lorenzo A ^a  

^a UNIVERSITY OF PADOVA   (Italy)

^b CA' FOSCARI UNIVERSITY OF VENICE   (Italy)

Author keywords

Apoptosis; ATP competitive inhibitors; CK2 mutants; Neoplasia; Protein kinase CK2

Indexed keywords

2 DIMETHYLAMINO 4,5,6,7 TETRABROMO 1H BENZIMIDAZOLE; 4,5,6,7 TETRABROMO 1H BENZOTRIAZOLE; 8 HYDROXY 4 METHYL 9 NITROBENZO[G]CHROMEN 2 ONE; [5 OXO 5,6 DIHYDROINDOLO (1,2A)QUINAZOLIN 7 YL]ACETIC ACID; ADENOSINE TRIPHOSPHATE; CASEIN KINASE II; EMODIN; GUANOSINE TRIPHOSPHATE; PROTEIN KINASE INHIBITOR; QUERCETIN; UNCLASSIFIED DRUG;

APOPTOSIS; ARTICLE; CELL MEMBRANE PERMEABILITY; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG BINDING SITE; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; PLEIOTROPY; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; TUMOR CELL;

ADENOSINE TRIPHOSPHATE; ANTINEOPLASTIC AGENTS; APOPTOSIS; BENZIMIDAZOLES; BINDING SITES; CASEIN KINASE II; CELL LINE; CELL MEMBRANE PERMEABILITY; COUMARINS; HOLOENZYMES; HUMANS; LIGANDS; MUTATION; PROTEIN KINASE INHIBITORS; QUINAZOLINES; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZOLES;

EID: 22344454956     PISSN: 03008177     EISSN: None     Source Type: Journal    
DOI: 10.1007/s11010-005-3079-z     Document Type: Article

References (36)

1. Pinna LA: Protein kinase CK2: A challenge to canons. J Cell Sci 115: 3873-3878, 2002. 12244125
2. Litchfield DW: Protein kinase CK2: Structure, regulation and the role in cellular decisions of life and death. Biochem J 369: 1-15, 2003. 12396231
3. Johnson LN, Noble ME, Owen DJ: Active and inactive protein kinases, structural basis for regulation. Cell 85: 149-158, 1996. 8612268
4. Niefind K, Guerra B, Pinna LA, Issinger O-G, Schomburg D: Crystal structure of the catalytic subunit of protein kinase CK2 from Zea mays at 2.1 A resolution. Embo J 17: 2451-2462, 1998. 9564028
5. Sarno S, Ghisellini P, Pinna LA: Unique activation mechanism of protein kinase CK2. The N-terminal segment is essential for constitutive activity of the catalytic subunit but not of the holoenzyme. J Biol Chem 277: 22509-22514, 2002. 11956194
6. Meggio F, Pinna LA: One-thousand-and-one substrates of protein kinase CK2? Faseb J 17: 349-368, 2003. 12631575
7. Tawfic S, Yu S, Wang H, Faust R, Davis A, Ahmed K: Protein kinase CK2 signal in neoplasia. Histol Histopathol 16: 573-582, 2001. 11332713
8. Seldin DC, Leder P: Casein kinase IIα transgene-induced murine lymphoma: Relation to Theileriosis in cattle. Science 267: 894-897, 1995. 7846532
9. Kelliher MA, Seldin DC, Leder P: Tal-1 induces T cell acute lymphoblastic leukemia accelerated by casein kinase IIα EMBO J 15: 5160-5166, 1996. 8895560
10. Landesman-Bolag E, Channavajhala PL, Cardiff RD, Seldin DC: P53 deficiency and misexpression of protein kinase CK2 alpha collaborate in the development of thymic lymphomas in mice. Oncogene 16: 2965-2974, 1998. 9662328
11. Faust RA, Gapany M, Tristani P, Davis A, Adams G, Ahmed K: Elevated protein kinase CK2 activity in chromatin of head and neck tumors: Association with malignant transformation. Cancer Lett 101: 31-35, 1996. 8625279
12. Guo C, Yu S, Davis AT, Wang H, Green JE, Ahmed K: A potential role of nuclear matrix-associated protein kinase CK2 in protection against drug-induced apoptosis in cancer cells. J Biol Chem 276: 5992-5999, 2001. 11069898
13. Ljubimov AV, Caballero S, Aoki AM, Pinna LA, Grant MB, Castellon R: Involvement of protein kinase CK2 in angiogenesis and retinal neovascularization. Invest Ophthalmol Vis Sci 45: 4583-4591, 2004. 15557471
14. Vangrevelinghe E, Zimmermann K, Schoepfer J, Portmann R, Fabbro D, Furet P: Discovery of a potent and selective protein kinase CK2 inhibitor by high-throughput docking. J Med Chem 46: 2656-2662, 2003. 12801229
15. Davalli S; Lunazzi L, Macciantelli D: Conformational studies by dynamic NMR. 40. Conformational atropoisomerism in highly hindered naphthylamines. J Org Chem 56: 1739-1747, 1991
16. Ohno A, Kunitomo J, Kawai Y, Kawamoto T, Tomishima M, Yoneda F: Atropisomeric flavoenzyme models with a modified pyrimidine ring: Synthesis, physical properties and stereochemistry in the reaction with NAD(P)H analogs. J Org Chem 61: 9344-9355, 1996
17. Meggio F, Pagano MA, Moro S, Zagotto G, Ruzzene M, Sarno S, Cozza G, Bain J, Elliott M, Donella-Deana A, Brunati AM, Pinna LA: Inhibition of protein kinase CK2 by condensed polyphenolic derivatives. An in vitro and in vivo study. Biochemistry 43: 12931-12936, 2004. 15461466
18. Pagano MA, Andrzejewska M, Ruzzene M, Sarno S, Cesaro L, Bain J, Elliott M, Meggio F, Kazimierczuk Z, Pinna LA: Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem 47: 6239-6247, 2004. 15566294
19. Sarno S, Vaglio P, Meggio F, Issinger O-G, Pinna LA: Protein kinase CK2 mutants defective in substrate recognition. Purification and kinetic analysis. J Biol Chem 271: 10595-10601, 1996. 8631861
20. Sarno S, De Moliner E, Ruzzene M, Pagano MA, Battistutta R, Bain J, Fabbro D, Schoepfer J, Elliott M, Furet P, Meggio F, Zanotti G, Pinna LA: Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2a)quinazolin-7-yl]acetic acid (IQA). Biochem J 374: 639-646, 2003. 12816539
21. 50: A more general use for the Dixon plot. J Chem Educ 80: 214-218, 2003
22. Zhang L, Lau Y-K, Xi L, Hong R-L, Kim DS, Chen C-F, Hortobagyi GN, Chang C, Hung M-C: Tyrosine kinase inhibitors, emodin and its derivative repress HER-2/neu-induced cellular transformation and metastasis-associated properties. Oncogene 16: 2855-2863, 1998. 9671406
23. Sarno S, Reddy H, Meggio F, Ruzzene M, Davies SP, Donella-Deana A, Shugar D, Pinna LA: Selectivity of 4,5,6,7-tetrabromobenzotriazole, an ATP site-directed inhibitor of protein kinase CK2 ("casein kinase-2"). FEBS Lett 496: 44-48, 2001. 11343704
24. Pagano MA, Meggio F, Ruzzene M, Andrzejewska M, Kazimierczuk Z, Pinna, LA: 2-Dimethylamino-4,5,6,7-terabromo-1H-benzimidazole: A novel powerful and selective inhibitor of protein kinase CK2. Biochem Biophys Res Commun 321: 1040-1044, 2004. 15358133
25. Battistutta R, Sarno S, De Moliner E, Papinutto E, Zanotti G, Pinna LA: The replacement of ATP by the competitive inhibitor emodin induces conformational modifications in the catalytic site of protein kinase CK2. J Biol Chem 275: 29618-29622, 2000. 10882732
26. Battistutta R, De Moliner E, Sarno S, Zanotti G, Pinna LA: Structural features underlying selective inhibition of protein kinase CK2 by ATP site-directed tetrabromo-2-benzotriazole. Protein Sci 10: 2200-2206, 2001. 11604527
27. De Moliner E, Moro S, Sarno S, Zagotto G, Zanotti G, Pinna LA, Battistutta R: Inhibition of protein kinase CK2 by anthraquinone-related compounds. A structural insight. J Biol Chem 278: 1831-1836, 2003. 12419810
28. Battistutta R, Sarno S, Zanotti G: Inhibitors of protein kinase CK2: Structural aspects. In: L.A. Pinna, T.W. Cohen (eds). Handbook of Experimental Pharmacology, Vol. 167, 2005, pp. 125-155
29. Ruzzene M, Penzo D, Pinna LA: Protein kinase CK2 inhibitor 4,5,6,7-tetrabromobenzotriazole (TBB) induces apoptosis and caspase-dependent degradation of haematopoietic lineage cell-specific protein 1 (HS1) in Jurkat cells. Biochem J 364: 41-47, 2002. 11988074
30. Loizou JI, El-Khamisy SF, Zlatanou A, Moore DJ, Chan DW, Qin J, Sarno S, Meggio F, Pinna LA, Caldecott KW: The protein kinase CK2 facilitates repair of chromosomal DNA single-strand breaks. Cell 117: 17-28, 2004. 15066279
31. Schwartz EI, Intine RV, Maraia RJ: CK2 is responsible for phosphorylation of human La protein serine-366 and can modulate rpL37 5′-Terminal oligopyrimidine mRNA metabolism. Mol Cell Biol 24: 9580-9591, 2004. 15485924
32. Kulartz M, Hiller E, Kappes F, Pinna LA, Knippers R: Protein kinase CK2 phosphorylates the cell cycle regulatory protein Geminin. Biochem Biophys Res Commun 315: 1011-1017, 2004. 14985113
33. Miyata Y, Nishida E: CK2 controls multiple protein kinases by phosphorylating a kinase-targeting molecular chaperone, cdc37. Mol Cell Biol 24: 4065-4074, 2004. 15082798
34. Marchetta M, Gamberi T, Sarno S, Magherini F, Raugei G, Camici G, Pinna LA, Modesti A: Expression of the Stp1 LMW-PTP and inhibition of protein kinase CK2 display a cooperative effect on immunophilin Fpr3 tyrosine phosphorylation and Saccharomyces cerevisiae growth. Cell Mol Life Sci 61: 1176-1184, 2004. 15141303
35. Kappes F, Damoc C, Knippers R, Przybylski M, Pinna LA, Gruss C: Phosphorylation by protein kinase CK2 changes the DNA binding properties of the human chromatin protein DEK. Mol Cell Biol 24: 6011-6020, 2004. 15199154
36. Mishra S, Reichert A, Cunnick J, Senadheera D, Hemmeryckx B, Heisterkamp N, Groffen J: Protein kinase CKIIalpha interacts with the Bcr moiety of Bcr/Abl and mediates proliferation of Bcr/Abl expressing cells. Oncogene 22: 8255-8262, 2003. 14614449