An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage

Cancer Research

Volumn 60, Issue 3, 2000, Pages 566-572

  Jackson, Jeffrey R ^a   Gilmartin, Aidan ^a   Imburgia, Christina ^a   Winkler, James D ^a   Marshall, Lisa A ^a   Roshak, Amy ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

INDOLOCARBAZOLE; PROTEIN KINASE INHIBITOR; SB 218078; UNCLASSIFIED DRUG;

ARTICLE; CANCER INHIBITION; CELL CULTURE; CELL CYCLE G2 PHASE; CYTOTOXICITY; DNA DAMAGE; DNA REPAIR; DRUG MECHANISM; ENZYME ACTIVITY; HUMAN; HUMAN CELL; PRIORITY JOURNAL;

ALKALOIDS; CELL CYCLE; DNA DAMAGE; DNA TOPOISOMERASES, TYPE I; ENZYME INHIBITORS; G2 PHASE; HUMANS; PROTEIN KINASE INHIBITORS; PROTEIN KINASES; TOPOTECAN;

EID: 0033975054     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (41)

1. 2 phase checkpoints. Cancer Surveys, 29: 151-182, 1997.
2. Carr, A. M. Checkpoints take the next step. Science (Washington DC), 271: 314-315, 1996.
3. Aldridge, D. R., and Radford, I. R. Explaining differences in sensitivity to killing by ionizing radiation between human lymphoid cell lines. Cancer Res., 58: 2817-2824, 1998.
4. Maity, A., McKenna, W. G., and Muschel, R. J. The molecular basis for cell cycle delays following ionizing radiation: a review. Radiother. Oncol., 31: 1-13, 1994.
5. Kastan, M. B., Onyekwere, O., Sidransky, D., Vogelstein, B., and Craig, RW Participation of p53 protein in the cellular response to DNA damage. Cancer Res., 51: 6304-6311, 1991.
6. Lau, C. C., and Pardee, A. B. Mechanism by which caffeine potentiates lethality of nitrogen mustard. Proc. Natl. Acad. Sci. USA, 79: 2942-2946, 1982.
7. 2 checkpoint function in cancer cells with disrupted p53. J. Natl. Cancer Inst., 88: 956-965, 1996.
8. Akinaga, S., Nomura, K., Gomi, K., and Okabe, M. Enhancement of antitumor activity of mitomycin C in vitro and in vivo by UCN-01, a selective inhibitor of protein kinase C. Cancer Chemother. Pharmacol., 32: 183-189, 1993.
9. 2-checkpoint inhibitor. Clin. Cancer Res., 2: 791-797, 1996.
10. Shao, R. G., Cao, C. X., Shimizu, T., O'Connor, P. M., Kohn, K. W., and Pommier, Y. Abrogation of an S-phase checkpoint and potentiation of camptothecin cytotoxicity by 7-hydroxystaurosporine (UCN-01) in human cancer cell lines, possibly influenced by p53 function. Cancer Res., 57: 4029-4035, 1997.
11. Fattaey, A., and Booher, R. N. Myt1: a Wee1-type kinase that phosphorylates Cdc2 on residue Thr14. Prog. Cell Cycle Res., 3: 233-240, 1997.
12. Walworth, N., Davey, S., and Beach, D. Fission yeast chk1 protein kinase links the rad checkpoint pathway to cdc2. Nature (Lond.), 363: 368-371, 1993.
13. Carr, A. M., Moudjou, M., Bentley, N. J., and Hagan, I. M. The chk1 pathway is required to prevent mitosis following cell-cycle arrest at 'start'. Curr. Biol., 5: 1179-1190, 1995.
14. Kumagai, A., Guo, Z., Emami, K. H., Wang, S. X., and Dunphy, W. G. The Xenopus Chk1 protein kinase mediates a caffeine-sensitive pathway of checkpoint control in cell-free extracts. J. Cell Biol., 142: 1559-1569, 1998.
15. Sanchez, Y., Wong, C., Thoma, R. S., Richman, R., Wu, Z., Piwnica-Worms, H., and Elledge, SJ Conservation of the Chk1 checkpoint pathway in mammals: linkage of DNA damage to Cdk regulation through Cdc25. Science (Washington DC), 277: 1497-1501, 1997.
16. 2 checkpoint control: regulation of 14-3-3 protein binding by phosphorylation of Cdc25C on serine-216. Science (Washington DC), 277: 1501-1505, 1997.
17. Mccombie, S. W., Bishop, R. W., Carr, D., Dobek, E., Kirkup, M. P., Kirschmeier, P., Lin, S. I., Petrin, J., Rosinski, K., Shankar, B. B., and Wilson, O. Indolocarbazoles 1: total synthesis and protein kinase inhibiting characteristics of compounds related to k-252c. Bioorg. Med. Chem. Lett., 3: 1537-1542, 1993.
18. Kingsbury, W. D., Boehm, J. C., Jakas, D. R., Holden, K. G., Hecht, S. M., Gallagher, G., Caranfa, M. J., McCabe, F. L., Faucette, L. F., and Johnson, R. K. Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity. J. Med. Chem., 34: 98-107, 1991.
19. Vindelov, L. L., Christensen, I. J., and Nissen, N. I. A detergent-trypsin method for the preparation of nuclei for flow cytometric DNA analysis. Cytometry, 3: 323-327, 1983.
20. Scudiero, D. A., Shoemaker, R. H., Paull, K. D., Monks, A., Tierney, S., Nofziger, T. H., Currens, M. J., Seniff, D., and Boyd, M. R. Evaluation of a soluble tetrazolium/ formazan assay for cell growth and drug sensitivity in culture using human and other tumor cell lines. Cancer Res., 48: 4827-4833, 1988.
21. Mackey, M. A., Morgan, W. F., and Dewey, W. C. Nuclear fragmentation and premature chromosome condensation induced by heat shock in S-phase Chinese hamster ovary cells. Cancer Res., 48: 6478-6483, 1988.
22. Bit, R. A., Davis, P. D., Elliott, L. H., Harris, W., Hill, C. H., Keech, E., Kumar, H., Lawton, G., Maw, A., Nixon, J. S., Vesey, D. R., Wadsworth, J., and Wilkinson, S. E. Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. J. Med. Chem., 36: 21-29, 1993.
23. Birchall, A. M., Bishop, J., Bradshaw, D., Cline, A., Coffey, J., Elliott, L. H., Gibson, V. M., Greenham, A., Hallam, T. J., Harris, W., Hill, C. H., Hutchings, A., Lamont, A. G., Lawton, G., Lewis, E. J., Maw, A., Nixon, J. S., Pole, D., Wadsworth, J., and Wilkinson, S. E. Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation. J. Pharmacol. Exp. Therap., 268: 922-929, 1994.
24. Ianzini, F., and Mackey, M. A. Spontaneous premature chromosome condensation and mitotic catastrophe following irradiation of HeLa S3 cells. Int. J. Radiat. Biol., 72: 409-421, 1997.
25. O'Connor, P. M., and Fan, S. DNA damage checkpoints: implications for cancer therapy. Prog. Cell Cycle Res., 2: 165-173, 1996.
26. Demarcq, C., Bunch, R. T., Creswell, D., and Eastman, A. The role of cell cycle progression in cisplatin-induced apoptosis in Chinese hamster ovary cells. Cell Growth Differ., 5: 983-993, 1994.
27. 1 checkpoint-competent cells. Cancer Res., 55: 1639-1642, 1995.
28. Nakamura, K., and Antoku, S. Enhancement of X-ray cell killing in cultured mammalian cells by the protein phosphatase inhibitor calyculin A. Cancer Res., 54: 2088-2090, 1994.
29. Tam, S. W., and Schlegel, R. Staurosporine overrides checkpoints for mitotic onset in BHK cells. Cell Growth Differ., 3: 811-817, 1992.
30. 2 block caused by staurosporine, a potent inhibitor of protein kinases. Exp. Cell Res., 192: 122-127, 1991.
31. 2 checkpoint inhibitors and identification of the structurally novel compound isogranulatimide. Cancer Res., 58: 5701-5706, 1998.
32. Boddy, M. N., Furnari, B., Mondesert, O., and Russell, P. Replication checkpoint enforced by kinases Cds1 and Chk1. Science (Washington DC), 280: 909-912, 1998.
33. Matsuoka, S., Huang, M., and Elledge, S. J. Linkage of ATM to cell cycle regulation by the Chk2 protein kinase. Science (Washington DC), 282: 1893-1897, 1998.
34. Blasina, A., de Weyer, I. V., Laus, M. C., Luyten, W. H., Parker, A. E., and McGowan, C. H. A human homologue of the checkpoint kinase Cds1 directly inhibits Cdc25 phosphatase. Curr. Biol., 9: 1-10, 1999.
35. Brown, A. L., Lee, C. H., Schwarz, J. K., Mitiku, N., Piwnica-Worms, H., and Chung, J. H. A human Cds1-related kinase that functions downstream of ATM protein in the cellular response to DNA damage. Proc. Natl. Acad. Sci. USA, 96: 3745-3750, 1999.
36. Chaturvedi, P., Eng, W. K., Zhu, Y., Mattern, M. R., Mishra, R., Hurle, M. R., Zhang, X., Annan, R. S., Lu, Q., Faucette, L. F., Scott, G. F., Li, X., Carr, S. A., Johnson, R. K., Winkler, J. D., and Zhou, B-B. S. Mammalian Chk2 is a downstream effector of the ATM-dependent DNA damage checkpoint pathway. Oncogene, 18: 4047-4054, 1999.
37. Chen, L., Liu, T. H., and Walworth, N. C. Association of Chk1 with 14-3-3 proteins is stimulated by DNA damage. Genes Dev., 13: 675-685, 1999.
38. Peng, C. Y., Graves, P. R., Ogg, S., Thoma, R. S., Byrnes, M. J., Wu, Z., Stephenson, M. T., and Piwnica-Worms, H. C-TAK1 protein kinase phosphorylates human Cdc25C on serine 216 and promotes 14-3-3 protein binding. Cell Growth Differ., 9: 197-208, 1998.
39. Meijer, L., and Kim, S. H. Chemical inhibitors of cyclin-dependent kinases. Methods Enzymol., 283: 113-128, 1997.
40. Chan, J. A., Freyer, A. J., Carte, B. K., Hemling, M. E., Hofmann, G. A., Mattern, M. R., Mentzer, M. A., and Westley, J. W. Protein kinase C inhibitors: novel spirosesquiterpene aldehydes from a marine sponge aka Siphonodictyon coralliphagum. J. Natural Prod., 57: 1543-1548, 1994.
41. Takahashi, I., Kobayashi, E., Asano, K., Yoshida, M., and Nakano, H. UCN-01, a selective inhibitor of protein kinase C from Streptomyces. J. Antibiot. (Tokyo), 40: 1782-1784, 1987.