The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4

Clinical Cancer Research

Volumn 5, Issue 12, 1999, Pages 4279-4286

  Kubo, Akihito ^a   Nakagawa, Kazuhiko ^a,d   Varma, Ravi K ^a   Conrad, Nicholas K ^a   Cheng, Jin Quan ^b   Lee, Wen Ching ^b   Testa, Joseph R ^b   Johnson, Bruce E ^a   Kaye, Frederic J ^a   Kelley, Michael J ^c,e  

^a NATIONAL CANCER INSTITUTE   (United States)

^b FOX CHASE CANCER CENTER   (United States)

^c DUKE UNIVERSITY MEDICAL CENTER   (United States)

^d KINKI UNIVERSITY SCHOOL OF MEDICINE   (Japan)

^e DURHAM VA MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIN DEPENDENT KINASE 4; PROTEIN P16;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER GROWTH; COMPETITIVE INHIBITION; ENZYME INHIBITION; ENZYME SPECIFICITY; GENE DELETION; GROWTH INHIBITION; HUMAN; HUMAN CELL; POINT MUTATION; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; RETINOBLASTOMA; TRANSCRIPTION REGULATION; TUMOR CELL LINE; TUMOR SUPPRESSOR GENE;

ANTINEOPLASTIC AGENTS; CYCLIN-DEPENDENT KINASE 4; CYCLIN-DEPENDENT KINASE INHIBITOR P16; CYCLIN-DEPENDENT KINASES; DRUG SCREENING ASSAYS, ANTITUMOR; ENZYME INHIBITORS; GENES, P16; GROWTH INHIBITORS; HUMANS; POLYMERASE CHAIN REACTION; POLYMORPHISM, SINGLE-STRANDED CONFORMATIONAL; PROTO-ONCOGENE PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; TUMOR CELLS, CULTURED;

EID: 0033386504     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (37)

1. Serrano, M., Hannon, G. J., and Beach, D. A new regulatory motif in cell-cycle control causing specific inhibition of cyclin D/CDK4. Nature (Lond.), 366: 704-707, 1993.
2. Weinberg, R. A. The relinoblastoma protein and cell cycle control. Cell, 81: 323-330, 1995.
3. Sellers, W. R., and Kaelin, W. G., Jr. Role of the retinoblastoma protein in the pathogenesis of human cancer. J. Clin. Oncol., 15: 3301-3312, 1997.
4. Liggett, W. H., Jr., and Sidransky, D. Role of the p16 tumor suppressor gene in cancer. J. Clin. Oncol., 16: 1197-1206, 1998.
5. Baylin, S. B., Herman, J. G., Graff, J. R., Vertino, P. M., and Issa, J. P. Alterations in DNA methylation: a fundamental aspect of neoplasia. Adv. Cancer Res., 72: 141-196, 1998.
6. Otterson, G. A., Kratzke, R. A., Coxon, A., Kim, Y. W., and Kaye, F. J. Absence of p16INK4 protein is restricted to the subset of lung cancer lines that retains wildtype RB. Oncogene, 9: 3375-3378, 1994.
7. Geradts, J., Kratzke, R. A., Niehans, G. A., and Lincoln, C. E. Immunohistochemical detection of the cyclin-dependent kinase inhibitor 2/multiple tumor suppressor gene 1 (CDKN2/MTS1) product p16INK4A in archival human solid tumors: correlation with retinoblastoma protein expression. Cancer Res., 55: 6006-6011, 1995.
8. Ueki, K., Ono, Y., Henson, J. W., Efird, J. T., von Deimling, A., and Louis, D. N. CDKN2/p16 or RB alterations occur in the majority of glioblastomas and are inversely correlated. Cancer Res., 56: 150-153, 1996.
9. Lukas, J., Parry, D., Aagaard, L., Mann, D. J., Bartkova, J., Strauss, M., Peters, G., and Bartek, J. Retinoblastoma-protein-dependent cell-cycle inhibition by the tumour suppressor p16. Nature (Lond.), 375: 503-506, 1995.
10. Guan, K. L., Jenkins, C. W., Li, Y., Nichols, M. A., Wu, X., O'Keefe, C. L., Matera, A. G., and Xiong, Y. Growth suppression by p18, a p16INK4/MTS1- and p14INK4B/MTS2-related CDK6 inhibitor, correlates with wild-type pRb function. Genes Dev., 8: 2939-2952, 1994.
11. Okamoto, A., Demetrick, D. J., Spillare, E. A., Hagiwara, K., Hussain, S. P., Bennett, W. P., Forrester, K., Gerwin, B., Serrano, M., Beach, D. H., and Harris, C. C. Mutations and altered expression of p16INK4 in human cancer. Proc. Natl. Acad. Sci. USA, 91: 11045-1109, 1994.
12. Liggett, W. H., Jr., Sewell, D. A., Rocco, J., Ahrendt, S. A., Koch, W., and Sidransky, D. p16 and p16 β are potent growth suppressors of head and neck squamous carcinoma cells in vitro. Cancer Res., 56: 4119-4123, 1996.
13. Jin, X., Nguyen, D., Zhang, W. W., Kyritsis, A. P., and Roth, J. A. Cell cycle arrest and inhibition of tumor cell proliferation by the p16INK4 gene mediated by an adenovirus vector. Cancer Res., 55: 3250-3253, 1995.
14. Sherr, C. J. Cancer cell cycles. Science (Washington DC), 274: 1672-1677, 1996.
15. Losiewicz, M. D., Carlson, B. A., Kaur, G., Sausville, E. A., and Worland, P. J. Potent inhibition of CDC2 kinase activity by the flavonoid L86-8275. Biochem. Biophys. Res. Commun., 201: 589-595, 1994.
16. Kitagawa, M., Okabe, T., Ogino, H., Matsumoto, H., Suzuki-Takahashi, I., Kokubo, T., Higashi, H., Saitoh, S., Taya, Y., Yasuda, H., Ohba, Y., Nishimura, S., Tanaka, N., and Okuyama, A. Butyrolactone I, a selective inhibitor of cdk2 and cdc2 kinase. Oncogene, 8: 2425-2432, 1993.
17. Gray, N. S., Wodicka, L., Thunnissen, A. M., Norman, T. C., Kwon, S., Espinoza, F. H., Morgan, D. O., Barnes, G., LeClerc, S., Meijer, L., Kim, S. H., Lockhart, D. J., and Schultz, P. G. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science (Washington DC), 281: 533-538, 1998.
18. Meijer, L., and Kim, S. H. Chemical inhibitors of cyclin-dependent kinases. Methods Enzymol., 283: 113-128, 1997.
19. Fahraeus, R., Lain, S., Ball, K. L., and Lane, D. P. Characterization of the cyclin-dependent kinase inhibitory domain of the INK4 family as a model for a synthetic tumour suppressor molecule. Oncogene, 16: 587-596, 1998.
20. Cohen, B. A., Colas, P., and Brent, R. An artificial cell-cycle inhibitor isolated from a combinatorial library. Proc. Natl. Acad. Sci. USA, 95: 14272-14277, 1998.
21. Monks, A., Scudiero, D., Skehan, P., Shoemaker, R., Paull, K., Vistica, D., Hose, C., Langley, J., Cronise, P., Vaigro-Wolff, A., Gray-Goodrich, M., Campbell, H., Mayo, J., and Boyd, M. Feasibility of a high-flux anticancer drug screen using a diverse panel of cultured human tumor cell lines. J. Natl. Cancer Inst., 83: 757-766. 1991.
22. Kelley, M. J., Nakagawa, K., Steinberg, S. M., Mulshine, J. L., Kamb, A., and Johnson, B. E. Differential inactivation of CDKN2 and Rb protein in non-small-cell and small-cell lung cancer cell lines. J. Natl. Cancer Inst., 87: 756-761, 1995.
23. Nakagawa, K., Conrad, N. K., Williams, J. P., Johnson, B. E., and Kelley, M. J. Mechanism of inactivation of CDKN2 and MTS2 in non-small cell lung cancer and association with advanced stage. Oncogene, 11: 1843-1851, 1995.
24. Kamb, A., Gruis, N. A., Weaver-Feldhaus, J., Liu, Q., Harshman, K., Tavtigian, S. V., Stockert, E., Day, R. S. R., Johnson, B. E., and Skolnick, M. H. A cell cycle regulator potentially involved in genesis of many tumor types. Science (Washington DC), 264: 436-440, 1994.
25. Paull, K. D., Shoemaker, R. H., Hodes, L., Monks, A., Scudiero, D. A., Rubinstein, L., Plowman, J., and Boyd, M. R. Display and analysis of patterns of differential activity of drugs against human tumor cell lines: Development of mean graph and COMPARE algorithm. J. Natl. Cancer Inst., 81: 1088-1092, 1989.
26. Alvarez, M., Paull, K., Monks, A., Hose, C., Lee, J. S., Weinstein, J., Grever, M., Bates, S., and Fojo, T. Generation of a drug resistance profile by quantitation of mdr-1/P- glycoprotein in the cell lines of the National Cancer Institute Anticancer Drug Screen. J. Clin. Investig., 95: 2205-2214, 1995.
27. Kitagawa, M., Higashi, H., Jung, H. K., Suzuki-Takahashi, I., Ikeda, M., Tamai, K., Kato, J., Segawa, K., Yoshida, E., Nishimura, S., and Taya, Y. The consensus motif for phosphorylation by cyclin D1-Cdk4 is different from that for phosphorylation by cyclin A/E-Cdk2. EMBO J., 15: 7060-7069, 1996.
28. Phelps, D. E., and Xiong, Y. Assay for activity of mammalian cyclin D-dependent kinases CDK4 and CDK6. Methods Enzymol., 283: 194-205, 1997.
29. Matsushime, H., Quelle, D. E., Shurtleff, S. A., Shibuya, M., Sherr. C. J., and Kato, J. Y. D-type cyclin-dependent kinase activity in mammalian cells. Mol. Cell. Biol., 14: 2066-2076, 1994.
30. Ranade, K., Hussussian, C. J., Sikorski, R. S., Varmus, H. E., Goldstein, A. M., Tucker, M. A., Serrano, M., Hannon, G. J., Beach, D., and Dracopoli, N. C. Mutations associated with familial melanoma impair p16INK4 function. Nat. Genet., 10: 114-116, 1995.
31. Pettit, G. R., Inoue, M., Kamano, Y., Herald, D. L., Arm, C., Dufresne, C., Christie, N. D., Schmidt, J. M., Doubeck, D. L., and Krupa, T. S. Isolation and structure of the powerful cell growth inhibition cephalostatin 1. J. Am. Chem. Soc., 110: 2006-2007, 1987.
32. Pettit, G. R., Herald, S. L., Doubek, D. L., Arnold, E., and Clardy, J. Isolation and structure of bryostatin 1. J. Am. Chem. Soc., 104: 6846-6848, 1982.
33. Kratzke, R. A., Otterson, G. A., Lincoln, C. E., Ewing, S., Oie, H., Geradts, J., and Kaye, F. J. Immunohistochemical analysis of the p16INK4 cyclin-dependent kinase inhibitor in malignant mesothelioma. J. Natl. Cancer Inst., 87: 1870-1875, 1995.
34. Kim, S. H. Structure-based inhibitor design for CDK2, a cell cycle controlling protein kinase. Pure Appl. Chem., 70: 555-565, 1998.
35. Russo, A. A., Tong, L., Lee, J. O., Jeffrey, P. D., and Pavletich, N. P. Structural basis for inhibition of the cyclin-dependent kinase Cdk6 by the tumour suppressor p16INK4a. Nature (Lond.), 395: 237-243, 1998.
36. Brotherton, D. H., Dhanaraj, V., Wick, S., Brizuela, L., Domaille, P. J., Volyanik, E., Xu, X., Parisini, E., Smith, B. O., Archer, S. J., Serrano, M., Brenner, S. L., Blundell, T. L., and Laue, E. D. Crystal structure of the complex of the cyclin D-dependent kinase Cdk6 bound to the cell-cycle inhibitor p19INK4d. Nature (Lond.), 395: 244-250, 1998.
37. Asiedu, C., Biggs, J., Lilly, M., and Kraft, A. S. Inhibition of leukemic cell growth by the protein kinase C activator bryostatin 1 correlates with the dephosphorylation of cyclin-dependent kinase 2. Cancer Res, 55: 3716-3720, 1995.