Parallel RNAi and compound screens identify the PDK1 pathway as a target for tamoxifen sensitization

Biochemical Journal

Volumn 417, Issue 1, 2009, Pages 361-370

  Iorns, Elizabeth ^a   Lord, Christopher J ^a   Ashworth, Alan ^a  

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

Author keywords

Chemical screen; Phosphoinositide dependent kinase 1 (PDK1); RNA interference screen; Tamoxifen; Tetrandrine; Triciribine

Indexed keywords

PHOSPHOINOSITIDE-DEPENDENT KINASE 1 (PDK1); RNA INTERFERENCE SCREEN; TAMOXIFEN; TETRANDRINE; TRICIRIBINE;

NUCLEIC ACIDS; RNA; TARGETS;

ELECTRIC RESISTANCE;

ANTIESTROGEN; ESTROGEN RECEPTOR ALPHA; PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1; PHOSPHOTRANSFERASE; PROTEIN DERIVATIVE; TAMOXIFEN; TETRANDRINE; TRICIRIBINE; BENZYLISOQUINOLINE DERIVATIVE; PROTEIN SERINE THREONINE KINASE; PYRUVATE DEHYDROGENASE (ACETYL TRANSFERRING) KINASE; PYRUVATE DEHYDROGENASE (ACETYL-TRANSFERRING) KINASE; RIBONUCLEOSIDE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG MECHANISM; DRUG SCREENING; DRUG TARGETING; ENZYME ANALYSIS; GENETIC SCREENING; HUMAN; HUMAN CELL; PRIORITY JOURNAL; RNA INTERFERENCE; CELL SURVIVAL; DRUG EFFECT; FLOW CYTOMETRY; GENETICS; METABOLISM; PHYSIOLOGY; SIGNAL TRANSDUCTION; TUMOR CELL LINE;

BENZYLISOQUINOLINES; CELL LINE, TUMOR; CELL SURVIVAL; ESTROGEN ANTAGONISTS; FLOW CYTOMETRY; HUMANS; PROTEIN-SERINE-THREONINE KINASES; RIBONUCLEOSIDES; RNA INTERFERENCE; SIGNAL TRANSDUCTION; TAMOXIFEN;

EID: 58249090328     PISSN: 02646021     EISSN: 14708728     Source Type: Journal    
DOI: 10.1042/BJ20081682     Document Type: Article

References (38)

1. Early Breast Cancer Trialists' Collaborative Group (1998) Tamoxifen for early breast cancer: an overview of the randomised trials. Early Breast Cancer Trialists' Collaborative Group. Lancet 351, 1451-1467
2. Cariou, S., Donovan, J. C., Flanagan, W. M., Milic, A., Bhattacharya, N. and Slingerland, J. M. (2000) Down-regulation of p21WAF1/CIP1 or p27Kip1 abrogates antiestrogen-mediated cell cycle arrest in human breast cancer cells. Proc. Natl. Acad. Sci. U.S.A. 97, 9042-9046
3. Musgrove, E. A., Lee, C. S., Buckley, M. F. and Sutherland, R. L. (1994) Cyclin D1 induction in breast cancer cells shortens G1 and is sufficient for cells arrested in G1 to complete the cell cycle. Proc. Natl. Acad. Sci. U.S.A. 91, 8022-8026
4. Ring, A. and Dowsett, M. (2004) Mechanisms of tamoxifen resistance. Endocr. Relat. Cancer 11, 643-658
5. Jordan, V. C. (1995) Third annual William L. McGuire Memorial Lecture. 'Studies on the estrogen receptor in breast cancer'-20 years as a target for the treatment and prevention of cancer. Breast Cancer Res. Treat. 36, 267-285
6. Iorns, E., Lord, C. J., Turner, N. and Ashworth, A. (2007) Utilizing RNA interference to enhance cancer drug discovery. Nat. Rev. Drug Discov. 6, 556-568
7. Iorns, E., Turner, N. C., Elliott, R., Syed, N., Garrone, O., Gasco, M., Tutt, A. N., Crook, T., Lord, C. J. and Ashworth, A. (2008) Identification of CDK10 as an important determinant of resistance to endocrine therapy for breast cancer. Cancer Cell 13, 91-104
8. Knight, Z. A. and Shokat, K. M. (2007) Chemical genetics: where genetics and pharmacology meet. Cell 128, 425-430
9. DiMasi, J. A., Hansen, R. W. and Grabowski, H. G. (2003) The price of innovation: new estimates of drug development costs. J. Health Econ. 22, 151-185
10. Abdi, H. (2007) Z-Scores, In Encyclopedia of Measurement and Statistics (Salkind, N., ed.), pp. 1-4, Sage, Thousand Oaks, CA
11. Chou, T. C. (2006) Theoretical basis, experimental design, and computerized simulation of synergism and antagonism in drug combination studies. Pharmacol. Rev. 58, 621-681
12. Mora, A., Komander, D., van Aalten, D. M. and Alessi, D. R. (2004) PDK1, the master regulator of AGC kinase signal transduction. Semin. Cell Dev. Biol. 15, 161-170
13. Chou, T. C. and Talalay, P. (1984) Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors. Adv. Enzyme Regul. 22, 27-55
14. Echeverri, C. J., Beachy, P. A., Baum, B., Boutros, M., Buchholz, F., Chanda, S. K., Downward, J., Ellenberg, J., Fraser, A. G., Hacohen, N. et al. (2006) Minimizing the risk of reporting false positives in large-scale RNAi screens. Nat. Methods 3, 777-779
15. Jones, S. E. (2002) A new estrogen receptor antagonist-an overview of available data. Breast Cancer Res. Treat. 75 (Suppl. 1), S19-S21; discussion S33-S15
16. Santen, R. J., Song, R. X., Zhang, Z., Kumar, R., Jeng, M. H., Masamura, S., Lawrence, Jr, J., MacMahon, L. P., Yue, W. and Berstein, L. (2005) Adaptive hypersensitivity to estrogen: mechanisms and clinical relevance to aromatase inhibitor therapy in breast cancer treatment. J. Steroid Biochem. Mol. Biol. 95, 155-165
17. Wilcken, N. R., Prall, O. W., Musgrove, E. A. and Sutherland, R. L. (1997) Inducible overexpression of cyclin D1 in breast cancer cells reverses the growth-inhibitory effects of antiestrogens. Clin. Cancer Res. 3, 849-854
18. Pestell, R. G., Albanese, C., Reutens, A. T., Segall, J. E., Lee, R. J. and Arnold, A. (1999) The cyclins and cyclin-dependent kinase inhibitors in hormonal regulation of proliferation and differentiation. Endocrin. Rev. 20, 501-534
19. Zhou, B. P., Liao, Y., Xia, W., Spohn, B., Lee, M. H. and Hung, M. C. (2001) Cytoplasmic localization of p21Cip1/WAF1 by Akt-induced phosphorylation in HER-2/neuoverexpressing cells. Nat. Cell Biol. 3, 245-252
20. Sheaff, R. J., Singer, J. D., Swanger, J., Smitherman, M., Roberts, J. M. and Clurman, B. E. (2000) Proteasomal turnover of p21Cip1 does not require p21Cip1 ubiquitination. Mol. Cell 5, 403-410
21. Chen, Y. J. (2002) Potential role of tetrandrine in cancer therapy. Acta Pharmacol. Sin. 23, 1102-1106
22. Xu, W. L., Shen, H. L., Ao, Z. F., Chen, B. A., Xia, W., Gao, F. and Zhang, Y. N. (2006) Combination of tetrandrine as a potential-reversing agent with daunorubicin, etoposide and cytarabine for the treatment of refractory and relapsed acute myelogenous leukemia. Leuk. Res. 30, 407-413
23. Chen, X. L., Ren, K. H., He, H. W. and Shao, R. G. (2008) Involvement of PI3K/AKT/GSK3β pathway in tetrandrine-induced G1 arrest and apoptosis. Cancer Biol. Ther. 7, 1073-1078
24. Fry, M. J. (2001) Phosphoinositide 3-kinase signalling in breast cancer: how big a role might it play? Breast Cancer Res. 3, 304-312
25. Lin, H. J., Hsieh, F. C., Song, H. and Lin, J. (2005) Elevated phosphorylation and activation of PDK-1/AKT pathway in human breast cancer. Br. J. Cancer 93, 1372-1381
26. Sabnis, G., Goloubeva, O., Jelovac, D., Schayowitz, A. and Brodie, A. (2007) Inhibition of the phosphatidylinositol 3-kinase/Akt pathway improves response of long-term estrogen-deprived breast cancer xenografts to antiestrogens. Clin. Cancer Res. 13, 2751-2757
27. Campbell, R. A., Bhat-Nakshatri, P., Patel, N. M., Constantinidou, D., Ali, S. and Nakshatri, H. (2001) Phosphatidylinositol 3-kinase/ AKT-mediated activation of estrogen receptor α: a new model for anti-estrogen resistance. J. Biol. Chem. 276, 9817-9824
28. Lu, C. H., Wyszomierski, S. L., Tseng, L. M., Sun, M. H., Lan, K. H., Neal, C. L., Mills, G. B., Hortobagyi, G. N., Esteva, F. J. and Yu, D. (2007) Preclinical testing of clinically applicable strategies for overcoming trastuzumab resistance caused by PTEN deficiency. Clin. Cancer Res. 13, 5883-5888
29. Balciunaite, E. and Kazlauskas, A. (2001) Early phosphoinositide 3-kinase activity is required for late activation of protein kinase Ci in platelet-derived-growth-factor-stimulated cells: evidence for signalling across a large temporal gap. Biochem. J. 358, 281-285
30. Hu, L., Zaloudek, C., Mills, G. B., Gray, J. and Jaffe, R. B. (2000) In vivo and in vitro ovarian carcinoma growth inhibition by a phosphatidylinositol 3-kinase inhibitor (LY294002). Clin. Cancer Res. 6, 880-886
31. Finan, P. M. and Thomas, M. J. (2004) PI 3-kinase inhibition: a therapeutic target for respiratory disease. Biochem. Soc. Trans. 32, 378-382
32. Cheng, J. Q., Lindsley, C. W., Cheng, G. Z., Yang, H. and Nicosia, S. V. (2005) The Akt/PKB pathway: molecular target for cancer drug discovery. Oncogene 24, 7482-7492
33. Schweinsberg, P. D., Smith, R. G. and Loo, T. L. (1981) Identification of the metabolites of an antitumor tricyclic nucleoside (NSC-154020). Biochem. Pharmacol. 30, 2521-2526
34. Feun, L. G., Blessing, J. A., Barrett, R. J. and Hanjani, P. (1993) A phase II trial of tricyclic nucleoside phosphate in patients with advanced squamous cell carcinoma of the cervix. A Gynecologic Oncology Group Study. Am. J. Clin. Oncol. 16, 506-508
35. Hoffman, K., Holmes, F. A., Fraschini, G., Esparza, L., Frye, D., Raber, M. N., Newman, R. A. and Hortobagyi, G. N. (1996) Phase I-II study: triciribine (tricyclic nucleoside phosphate) for metastatic breast cancer. Cancer Chemother. Pharmacol. 37, 254-258
36. He, Q. Y., Meng, F. H. and Zhang, H. Q. (1996) Reduction of doxorubicin resistance by tetrandrine and dauricine in harringtonine-resistant human leukemia (HL60) cells. Zhongguo Yao Li Xue Bao 17, 179-181
37. Chang, K. H., Chen, M. L., Chen, H. C., Huang, Y. W., Wu, T. Y. and Chen, Y. J. (1999) Enhancement of radiosensitivity in human glioblastoma U138MG cells by tetrandrine. Neoplasma 46, 196-200
38. Torbett, N. E., Luna, A., Knight, Z. A., Houk, A., Moasser, M., Weiss, W., Shokat, K. M. and Stokoe, D. (2008) A chemical screen in diverse breast cancer cell lines reveals genetic enhancers and suppressors of sensitivity to PI3K isotype-selective inhibition. Biochem. J. 415, 97-110