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Treatment of ER+ human breast cancer cell lines, MCF7 and T47D cells with fulvestrant caused a significant decrease in MDM2 protein expression. Treatment with fulvestrant for 16 h or 66 h does not alter MDM2 mRNA level. Fulvestrant (1 μM, 16 h) facilitated degradation of MDM2 protein and shortened half-life of this protein (27 min vs. 42 min in T47D cells; 80 min vs. 180 min in MCF7 cells). Treatment with fulvestrant (5 μM, 72 h) increased the G1 population.
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References:
[1] Dolfi SC1, Jger AV2, Medina DJ1, Haffty BG3, Yang JM4, Hirshfield KM5.Fulvestrant treatment alters MDM2 protein turnover and sensitivity of human breast carcinoma cells to chemotherapeutic drugs. Cancer Lett. 2014 Apr 18. pii: S0304-3835 (14) 00215-8.
[2] Wakeling A E, Dukes M, Bowler J. A potent specific pure antiestrogen with clinical potential [J]. Cancer research, 1991, 51 (15): 3867-3873.
[3] Howell A, Robertson J F R, Quaresma Albano J, et al. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment [J]. Journal of Clinical Oncology, 2002, 20 (16): 3396-3403.
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