DOI QR코드

DOI QR Code

The Effect of Selective Estrogen Receptor Modulators (SERMs) on the Tamoxifen Resistant Breast Cancer Cells

  • Chang, Bo-Yoon (Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University) ;
  • Kim, Sae-Am (Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University) ;
  • Malla, Bindu (Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University) ;
  • Kim, Sung-Yeon (Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University)
  • 투고 : 2011.05.08
  • 심사 : 2011.05.16
  • 발행 : 2011.06.01

초록

Selective estrogen receptor modulators (SERMs) are synthetic molecules which bind to estrogen receptors (ER) and can modulate its transcriptional capabilities in different ways in diverse estrogen target tissues. Tamoxifen, the prototypical SERM, is extensively used for targeted therapy of ER positive breast cancers. Unfortunately, the use of tamoxifen is associated with acquired resistance and some undesirable side effects. This study investigated the availability of the conventional SERMs on the TAM-resistance breast cancer cells. SERMs showed more effectiveness in MCF-7 cells than tamoxifen resistant cells, except toremifene and ospemifene. Especially, toremifene was more efficacious in tamoxifen resistant cells than MCF-7. Ospemifene had similar cytotoxic activity on the two types of breast cancers. The other SERMs used in this experiment didn't inhibit efficiently the proliferation of tamoxifen resistant cells. These results support the possibility to usage of toremifene on tamoxifen resistant cancer. The effectiveness by toremifene on tamoxifen resistant cells might be different pathways from the apoptosis and the autophagy. Further study should be needed to elucidate the underlying mechanism of effect of toremifene on tamoxifen resistant cancer.

키워드

참고문헌

  1. Adamo, V., Iorfida, M., Montalto, E., Festa, V., Garipoli, C., Scimone, A., Zanghì, M. and Caristi, N. (2007). Overview and new strategies in metastatic breast cancer (MBC) for treatment of tamoxifen-resistant patients. Ann. Oncol., 18 Suppl 6, 53-57.
  2. Avioli, L.V. (1999). SERM drugs for the prevention of osteoporosis. Trends. Endocrinol. Metab., 10, 317-319. https://doi.org/10.1016/S1043-2760(99)00176-9
  3. Berthou, F., Dreano, Y., Belloc, C., Kangas, L., Gautier, J.C. and Beaune, P. (1994). Involvement of cytochrome P450 3A enzyme family in the major metabolic pathways of toremifene in human liver microsomes. Biochem. Pharmacol., 47, 1883-1895. https://doi.org/10.1016/0006-2952(94)90319-0
  4. Chen, Y., Azad, M.B. and Gibson, S.B. (2009). Superoxide is the major reactive oxygen species regulating autophagy. Cell Death Differ., 16, 1040-1052. https://doi.org/10.1038/cdd.2009.49
  5. Chen, Y., Azad, M.B. and Gibson, S.B. (2010). Methods for detecting autophagy and determining autophagy-induced cell death. Can. J. Physiol. Pharmacol., 88, 285-295. https://doi.org/10.1139/Y10-010
  6. Choi, H.K., Yang, J.W., Roh, S.H., Han, C.Y. and Kang, K.W. (2007). Induction of multidrug resistance associated protein 2 in tamoxifen-resistant breast cancer cells. Endocr. Relat. Cancer, 14, 293-303. https://doi.org/10.1677/ERC-06-0016
  7. Coezy, E., Borgna, J.L. and Rochefort, H. (1982). Tamoxifen and metabolites in MCF7 cells: correlation between binding to estrogen receptor and inhibition of cell growth. Cancer Res., 42, 317-323.
  8. Cummings, S.R., Eckert, S., Krueger, K.A., Grady, D., Powles, T.J., Cauley, J.A., Norton, L., Nickelsen, T., Bjarnason, N.H., Morrow, M., Lippman, M.E., Black, D., Glusman, J.E., Costa, A. and Jordan, V.C. (1999). The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. Multiple outcomes of raloxifene evaluation. JAMA, 281, 2189-2197. https://doi.org/10.1001/jama.281.23.2189
  9. Dalby, K.N., Tekedereli, I., Lopez-Berestein, G. and Ozpolat, B. (2010). Targeting the prodeath and prosurvival functions of autophagy as novel therapeutic strategies in cancer. Autophagy, 6, 322-329. https://doi.org/10.4161/auto.6.3.11625
  10. Gonzalez-Malerva, L., Park, J., Zou, L., Hu, Y., Moradpour, Z., Pearlberg, J., Sawyer, J., Stevens, H., Harlow, E. and LaBaer, J. (2011). High-throughput ectopic expression screen for tamoxifen resistance identifies an atypical kinase that blocks autophagy. Proc. Natl. Acad. Sci. U.S.A., 108, 2058-2063. https://doi.org/10.1073/pnas.1018157108
  11. Jirecek, S., Pavo, I. and Huber, J.C. (1999). Effect of selective estrogen receptor modulators on estrogen-sensitive tissues. Gynakol Geburtshilfliche Rundsch, 39, 184-190. https://doi.org/10.1159/000022308
  12. Johnston, S.R. (2001). Endocrine manipulation in advanced breast cancer: recent advances with SERM therapies. Clin. Cancer Res., 7, 4376s-4387s.
  13. Jordan, V.C. (1988). Chemosuppression of breast cancer with tamoxifen: laboratory evidence and future clinical investigations. Cancer Invest., 6, 589-595. https://doi.org/10.3109/07357908809082124
  14. Kim, S.Y., Suzuki, N., Santosh Laxmi, Y.R., Rieger, R. and Shibutani, S. (2003). Alpha-hydroxylation of tamoxifen and toremifene by human and rat cytochrome P450 3A subfamily enzymes. Chem. Res. Toxicol., 16, 1138-1144. https://doi.org/10.1021/tx0300131
  15. Knowlden, J.M., Hutcheson, I.R., Jones, H.E., Madden, T., Gee, J.M., Harper, M.E., Barrow, D., Wakeling, A.E. and Nicholson, R.I. (2003). Elevated levels of epidermal growth factor receptor/c-erbB2 heterodimers mediate an autocrine growth regulatory pathway in tamoxifen-resistant MCF-7 cells. Endocrinology, 144, 1032-1044. https://doi.org/10.1210/en.2002-220620
  16. Labrie, F., El-Alfy, M., Berger, L., Labrie, C., Martel, C., Belanger, A., Candas, B. and Pelletier, G. (2003). The combination of a novel selective estrogen receptor modulator with an estrogen protects the mammary gland and uterus in a rodent model: the future of postmenopausal women's health? Endocrinology, 144, 4700-4706. https://doi.org/10.1210/en.2003-0269
  17. Lerner, L.J. and Jordan, V.C. (1990). Development of antiestrogens and their use in breast cancer: eighth Cain memorial award lecture. Cancer Res., 50, 4177-4189.
  18. Levenson, A.S. and Jordan, V.C. (1999). Selective oestrogen receptor modulation: molecular pharmacology for the millennium. Eur. J. Cancer., 35, 1974-1985. https://doi.org/10.1016/S0959-8049(99)00297-X
  19. Lin, J.P., Yang, J.S., Chang, N.W., Chiu, T.H., Su, C.C., Lu, K.W., Ho, Y.T., Yeh, C.C., Mei, D., Lin, H.J. and Chung, J.G. (2007). GADD153 mediates berberine-induced apoptosis in human cervical cancer Ca ski cells. Anticancer. Res., 27, 3379-3386.
  20. Malet, C., Gompel, A., Spritzer, P., Bricout, N., Yaneva, H., Mowszowicz, I., Kuttenn, F. and Mauvais-Jarvis, P. (1988). Tamoxifen and hydroxytamoxifen isomers versus estradiol effects on normal human breast cells in culture. Cancer Res., 48, 7193-7199.
  21. McCague, R., Leclercq, G., Legros, N., Goodman, J., Blackburn, G.M., Jarman, M. and Foster, A.B. (1989). Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent. J. Med. Chem., 32, 2527-2533. https://doi.org/10.1021/jm00132a006
  22. Miller, W.R., Bartlett, J.M., Canney, P. and Verrill, M. (2007). Hormonal therapy for postmenopausal breast cancer: the science of sequencing. Breast. Cancer Res. Treat., 103, 149-160. https://doi.org/10.1007/s10549-006-9369-7
  23. Morishima, S., Shibata, M.A., Ohmichi, M. and Otsuki, Y. (2008). Raloxifene, a selective estrogen receptor modulator, induces mitochondria-mediated apoptosis in human endometrial carcinoma cells. Med. Mol. Morphol., 41, 132-138. https://doi.org/10.1007/s00795-008-0403-1
  24. Normanno, N., Di Maio. M., De Maio, E., De Luca, A., de Matteis, A., Giordano, A., Perrone, F. and NCI-Naple Breast Cancer Group. (2005). Mechanisms of endocrine resistance and novel therapeutic strategies in breast cancer. Endocr. Relat. Cancer, 12, 721-747. https://doi.org/10.1677/erc.1.00857
  25. Osborne, C.K., Zhao, H. and Fuqua, S.A. (2000). Selective estrogen receptor modulators: structure, function, and clinical use. J. Clin. Oncol., 18, 3172-3186. https://doi.org/10.1200/JCO.2000.18.17.3172
  26. Pecorino, L. (2008). Molecular biology and cancer (2nd edition), Oxford University press, New York, pp 137-160.
  27. Peng, J., Sengupta, S. and Jordan, V.C. (2009). Potential of selective estrogen receptor modulators as treatments and preventives of breast cancer. Anticancer. Agents. Med. Chem., 9, 481-499. https://doi.org/10.2174/187152009788451833
  28. Purdie, D.W. and Beardsworth, S.A. (1999). The selective oestrogen receptor modulation: evolution and clinical applications. Br. J. Clin. Pharmacol., 48, 785-792.
  29. Rodriguez, L., Carrillo, M., Sorbera, L.A., Zohar, Y. and Zany, S. (2004). Effects of photoperiod on pituitary levels of three forms of GnRH and reproductive hormones in the male European sea bass (Dicentrarchus labrax, L.) during testicular differentiation and first testicular recrudescence. Gen. Comp. Endocrinol., 136, 37-48. https://doi.org/10.1016/j.ygcen.2003.11.010
  30. Samaddar, J.S., Gaddy, V.T., Duplantier, J., Thandavan, S.P., Shah, M., Smith, M.J., Browning, D., Rawson, J., Smith, S.B., Barrett, J.T. and Schoenlein, P.V. (2008). A role for macroautophagy in protection against 4-hydroxytamoxifen-induced cell death and the development of antiestrogen resistance. Mol. Cancer Ther., 7, 2977-2987. https://doi.org/10.1158/1535-7163.MCT-08-0447
  31. Schoenlein, P.V., Periyasamy-Thandavan, S., Samaddar, J.S., Jackson, W.H. and Barrett, J.T. (2009). Autophagy facilitates the progression of ERalpha-positive breast cancer cells to antiestrogen resistance. Autophagy, 5, 400-403. https://doi.org/10.4161/auto.5.3.7784
  32. Shelly, W., Draper, M.W., Krishnan, V., Wong, M. and Jaffe, R.B. (2008). Selective estrogen receptor modulators: an update on recent clinical findings. Obstet. Gynecol. Surv., 63, 163-181.
  33. Shibutani, S., Ravindernath, A., Terashima, I., Suzuki, N., Laxmi, Y.R., Kanno, Y., Suzuki, M., Apak, T.I., Sheng, J.J. and Duffel, M.W. (2001). Mechanism of lower genotoxicity of toremifene compared with tamoxifen. Cancer Res., 61, 3925-3931.
  34. Stearns, V., Johnson, M.D., Rae, J.M., Morocho, A., Novielli, A., Bhargava, P., Hayes, D.F., Desta, Z. and Flockhart, D.A. (2003). Active tamoxifen metabolite plasma concentrations after coadministration of tamoxifen and the selective serotonin reuptake inhibitor paroxetine. J. Natl. Cancer Inst., 95, 1758-1764. https://doi.org/10.1093/jnci/djg108
  35. Warri, A.M., Huovinen, R.L., Laine, A.M., Martikainen, P.M. and Härkönen, P.L. (1993). Apoptosis in toremifene-induced growth inhibition of human breast cancer cells in vivo and in vitro. J. Natl. Cancer Inst., 85, 1412-1418. https://doi.org/10.1093/jnci/85.17.1412

피인용 문헌

  1. Development of new estrogen receptor-targeting therapeutic agents for tamoxifen-resistant breast cancer vol.5, pp.9, 2013, https://doi.org/10.4155/fmc.13.63
  2. Comprehensive characterization of glioblastoma tumor tissues for biomarker identification using mass spectrometry-based label-free quantitative proteomics vol.46, pp.13, 2014, https://doi.org/10.1152/physiolgenomics.00034.2014