A novel Chk inhibitor, XL-844, increases human cancer cell radiosensitivity through promotion of mitotic catastrophe

Investigational New Drugs

Volumn 29, Issue 3, 2011, Pages 514-522

  Riesterer, Oliver ^a,b   Matsumoto, Fumihiko ^a   Wang, Li ^a   Pickett, Jessica ^a   Molkentine, David ^a   Giri, Uma ^a   Milas, Luka ^a   Raju, Uma ^a  

^a UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

^b UNIVERSITY HOSPITAL ZURICH   (Switzerland)

Author keywords

Inhibitor of Check point kinases; Mitotic catastrophe; Pan nuclear H2AX; Radiosensitivity; XL 844

Indexed keywords

ALPHA TUBULIN; ANTINEOPLASTIC AGENT; CHECKPOINT KINASE 1; CHECKPOINT KINASE 2; GAMMA TUBULIN; HISTONE H2AX; UNCLASSIFIED DRUG; XL 844;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CELL CYCLE; CELL STRAIN HT29; CELL SURVIVAL; CONTROLLED STUDY; DNA REPAIR; DOSE RESPONSE; DRUG CYTOTOXICITY; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; ENZYME PHOSPHORYLATION; FLOW CYTOMETRY; HUMAN; HUMAN CELL; IMAGE ANALYSIS; IMMUNOCYTOCHEMISTRY; MITOSIS SPINDLE; PRIORITY JOURNAL; RADIOSENSITIVITY; SIGNAL TRANSDUCTION; WESTERN BLOTTING;

ANTINEOPLASTIC AGENTS; APOPTOSIS; CELL LINE, TUMOR; HISTONES; HUMANS; IMMUNOHISTOCHEMISTRY; MITOSIS; PROTEIN KINASE INHIBITORS; PROTEIN KINASES; PROTEIN-SERINE-THREONINE KINASES; RADIATION TOLERANCE; SIGNAL TRANSDUCTION; TUBULIN;

EID: 79955623625     PISSN: 01676997     EISSN: None     Source Type: Journal    
DOI: 10.1007/s10637-009-9361-2     Document Type: Article

References (45)

1. Zhou BB, Elledge SJ (2000) The DNA damage response: putting checkpoints in perspective. Nature 408(6811):433-439
2. Banin S, Moyal L, Shieh S, Taya Y, Anderson CW, Chessa L, Smorodinsky NI, Prives C, Reiss Y, Shiloh Y, Ziv Y (1998) Enhanced phosphorylation of p53 by ATM in response to DNA damage. Science 281(5383):1674-1677
3. Canman CE, Lim DS, Cimprich KA, Taya Y, Tamai K, Sakaguchi K, Appella E, Kastan MB, Siliciano JD (1998) Activation of the ATM kinase by ionizing radiation and phosphorylation of p53. Science 281(5383):1677-1679 (Pubitemid 28435584)
4. Elledge SJ (1996) Cell cycle checkpoints: preventing an identity crisis. Science 274(5293):1664-1672
5. Painter RB, Young BR (1980) Radiosensitivity in ataxiatelangiectasia: a new explanation. Proc Natl Acad Sci USA 77 (12):7315-7317
6. Samuel T, Weber HO, Funk JO (2002) Linking DNA damage to cell cycle checkpoints. Cell Cycle 1(3):162-168
7. Chaturvedi P, Eng WK, Zhu Y, Mattern MR, Mishra R, Hurle MR, Zhang X, Annan RS, Lu Q, Faucette LF, Scott GF, Li X, Carr SA, Johnson RK, Winkler JD, Zhou BB (1999) Mammalian Chk2 is a downstream effector of the ATM-dependent DNA damage checkpoint pathway. Oncogene 18(28):4047-4054 (Pubitemid 29363911)
8. Pommier Y, Sordet O, Rao VA, Zhang H, Kohn KW (2005) Targeting chk2 kinase: molecular interaction maps and therapeutic rationale. Curr Pharm Des 11(22):2855-2872 (Pubitemid 41051871)
9. Bartek J, Falck J, Lukas J (2001) CHK2 kinase - a busy messenger. Nat Rev Mol Cell Biol 2(12):877-886 (Pubitemid 33674087)
10. Taylor WR, Stark GR (2001) Regulation of the G2/M transition by p53. Oncogene 20(15):1803-1815 (Pubitemid 32458690)
11. Choudhury A, Cuddihy A, Bristow RG (2006) Radiation and new molecular agents part I: targeting ATM-ATR checkpoints, DNA repair, and the proteasome. Semin Radiat Oncol 16(1):51-58 (Pubitemid 41832316)
12. Xu B, Kim ST, Lim DS, Kastan MB (2002) Two molecularly distinct G(2)/M checkpoints are induced by ionizing irradiation. Mol Cell Biol 22(4):1049-1059 (Pubitemid 34094842)
13. Matthews DJ, Yakes FM, Chen J, Tadano M, Bornheim L, Clary DO, Tai A, Wagner JM, Miller N, Kim YD, Robertson S, Murray L, Karnitz LM (2007) Pharmacological abrogation of S-phase checkpoint enhances the anti-tumor activity of gemcitabine in vivo. Cell Cycle 6(1):104-110 (Pubitemid 46173886)
14. Busby EC, Leistritz DF, Abraham RT, Karnitz LM, Sarkaria JN (2000) The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1. Cancer Res 60 (8):2108-2112 (Pubitemid 30225168)
15. Jobson AG, Lountos GT, Lorenzi PL, Llamas J, Connelly J, Cerna D, Tropea JE, Onda A, Zoppoli G, Kondapaka S, Zhang G, Caplen NJ, Cardellina JH, Yoo SS, Monks A, Self C, Waugh DS, Shoemaker RH, Pommier Y (2009) Cellular inhibition of Chk2 kinase and potentiation of camptothecins and radiation by the novel Chk2 inhibitor PV1019. J Pharmacol Exp Ther Epub ahead of print
16. Ashwell S, Janetka JW, Zabludoff S (2008) Keeping checkpoint kinases in line: new selective inhibitors in clinical trials. Expert Opin Investig Drugs 17(9):1331-1340
17. Fertil B, Malaise EP (1981) Inherent cellular radiosensitivity as a basic concept for human tumor radiotherapy. Int J Radiat Oncol Biol Phys 7(5):621-629 (Pubitemid 11072545)
18. Antoni L, Sodha N, Collins I, Garrett MD (2007) CHK2 kinase: cancer susceptibility and cancer therapy - two sides of the same coin? Nat Rev Cancer 7(12):925-936
19. Matsuoka S, Huang M, Elledge SJ (1998) Linkage of ATM to cell cycle regulation by the Chk2 protein kinase. Science 282 (5395):1893-1897 (Pubitemid 28555269)
20. Ahn JY, Schwarz JK, Piwnica-Worms H, Canman CE (2000) Threonine 68 phosphorylation by ataxia telangiectasia mutated is required for efficient activation of Chk2 in response to ionizing radiation. Cancer Res 60(21):5934-5936
21. Tse AN, Rendahl KG, Sheikh T, Cheema H, Aardalen K, Embry M, Ma S, Moler EJ, Ni ZJ, Lopes de Menezes DE, Hibner B, Gesner TG, Schwartz GK (2007) CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivo. Clin Cancer Res 13(2 Pt 1):591-602 (Pubitemid 46225366)
22. Xiao Z, Xue J, Sowin TJ, Rosenberg SH, Zhang H (2005) A novel mechanism of checkpoint abrogation conferred by Chk1 downregulation. Oncogene 24(8):1403-1411 (Pubitemid 40343120)
23. Ganzinelli M, Carrassa L, Crippa F, Tavecchio M, Broggini M, Damia G (2008) Checkpoint Kinase 1 down-regulation by an inducible small interfering RNA expression system sensitized in vivo tumors to treatment with 5-fluorouracil. Clin Cancer Res 14 (16):5131-5141
24. Koniaras K, Cuddihy AR, Christopoulos H, Hogg A, O'Connell MJ (2001) Inhibition of Chk1-dependent G2 DNA damage checkpoint radiosensitizes p53 mutant human cells. Oncogene 20(51):7453-7463 (Pubitemid 33086904)
25. Zhao H, Watkins JL, Piwnica-Worms H (2002) Disruption of the checkpoint kinase 1/cell division cycle 25A pathway abrogates ionizing radiation-induced S and G2 checkpoints. Proc Natl Acad Sci USA 99(23):14795-14800 (Pubitemid 35334563)
26. Yu Q, La Rose J, Zhang H, Takemura H, Kohn KW, Pommier Y (2002) UCN-01 inhibits p53 up-regulation and abrogates gamma-radiation-induced G(2)-M checkpoint independently of p53 by targeting both of the checkpoint kinases, Chk2 and Chk1. Cancer Res 62(20):5743-5748 (Pubitemid 35204730)
27. Atherton-Fessler S, Parker LL, Geahlen RL, Piwnica-Worms H (1993) Mechanisms of p34cdc2 regulation. Mol Cell Biol 13 (3):1675-1685
28. Galaktionov K, Lee AK, Eckstein J, Draetta G, Meckler J, Loda M, Beach D (1995) CDC25 phosphatases as potential human oncogenes. Science 269(5230):1575-1577
29. Norbury C, Nurse P (1992) Animal cell cycles and their control. Annu Rev Biochem 61:441-470
30. Watanabe N, Broome M, Hunter T (1995) Regulation of the human WEE1Hu CDK tyrosine 15-kinase during the cell cycle. Embo J 14(9):1878-1891
31. Hunter T (1995) Protein kinases and phosphatases: the yin and yang of protein phosphorylation and signaling. Cell 80(2):225-236
32. Kastan MB, Lim DS, Kim ST, Yang D (2001) ATM - a key determinant of multiple cellular responses to irradiation. Acta Oncol 40(6):686-688 (Pubitemid 33081975)
33. Raju U, Ariga H, Dittmann K, Nakata E, Ang KK, Milas L (2005) Inhibition of DNA repair as a mechanism of enhanced radio-response of head and neck carcinoma cells by a selective cyclooxygenase-2 inhibitor, celecoxib. Int J Radiat Oncol Biol Phys 63(2):520-528 (Pubitemid 41317170)
34. Syljuasen RG, Sorensen CS, Hansen LT, Fugger K, Lundin C, Johansson F, Helleday T, Sehested M, Lukas J, Bartek J (2005) Inhibition of human Chk1 causes increased initiation of DNA replication, phosphorylation of ATR targets, and DNA breakage. Mol Cell Biol 25(9):3553-3562 (Pubitemid 40559562)
35. Belmont LD, Hyman AA, Sawin KE, Mitchison TJ (1990) Real-time visualization of cell cycle-dependent changes in microtubule dynamics in cytoplasmic extracts. Cell 62(3):579-589
36. Eriksson D, Lofroth PO, Johansson L, Riklund KA, Stigbrand T (2007) Cell cycle disturbances and mitotic catastrophes in HeLa Hep2 cells following 2.5 to 10 Gy of ionizing radiation. Clin Cancer Res 13(18 Pt 2):5501s-5508s
37. McIntosh JR (1984) Cell biology.Microtubule catastrophe. Nature 312(5991):196-197
38. Robinson HM, Black EJ, Brown R, Gillespie DA (2007) DNA mismatch repair and Chk1-dependent centrosome amplification in response to DNA alkylation damage. Cell Cycle 6(8):982-992 (Pubitemid 46658753)
39. Castedo M, Perfettini JL, Roumier T, Yakushijin K, Horne D, Medema R, Kroemer G (2004) The cell cycle checkpoint kinase Chk2 is a negative regulator of mitotic catastrophe. Oncogene 23 (25):4353-4361 (Pubitemid 38850414)
40. Roninson IB, Broude EV, Chang BD (2001) If not apoptosis, then what? Treatment-induced senescence and mitotic catastrophe in tumor cells. Drug Resist Updat 4(5):303-313 (Pubitemid 34456384)
41. Cenciarelli C, Tanzarella C, Vitale I, Pisano C, Crateri P, Meschini S, Arancia G, Antoccia A (2008) The tubulin-depolymerising agent combretastatin-4 induces ectopic aster assembly and mitotic catastrophe in lung cancer cells H460. Apoptosis 13(5):659-669
42. Brown JM, Attardi LD (2005) The role of apoptosis in cancer development and treatment response. Nat Rev Cancer 5(3):231-237 (Pubitemid 40314954)
43. Niida H, Tsuge S, Katsuno Y, Konishi A, Takeda N, Nakanishi M (2005) Depletion of Chk1 leads to premature activation of Cdc2-cyclin B and mitotic catastrophe. J Biol Chem 280(47):39246-39252 (Pubitemid 41713877)
44. Mitchison T, KirschnerM(1984) Dynamic instability of microtubule growth. Nature 312(5991):237-242
45. Oakley CE, Oakley BR (1989) Identification of gamma-tubulin, a new member of the tubulin superfamily encoded by mipA gene of Aspergillus nidulans. Nature 338(6217):662-664 (Pubitemid 19104647)