Jordan Nicola J, Gee Julia M W, Barrow Denise, Wakeling Alan E, Nicholson Robert I
Tenovus Centre for Cancer Research, Welsh School of Pharmacy, Cardiff University, Cardiff, CF10 3XF, UK.
Breast Cancer Res Treat. 2004 Sep;87(2):167-80. doi: 10.1023/B:BREA.0000041623.21338.47.
The tamoxifen-resistant (TAM-R) MCF-7 breast cancer cell line has been used as a model to identify the signalling pathways that enable resistant cancer cells to grow independently of steroid hormones. In TAM-R cells, peptide growth factor signalling pathways appear to be important in modified cell behaviour, growth and survival. The PI3 kinase signalling components Akt1 and Akt2 are expressed at similar levels by both parental wild-type MCF-7 and TAM-R cells, but Akt1 phosphorylation is significantly increased in TAM-R cells grown under basal conditions. High levels of basal Akt, GSK3 alpha / beta and p70S6 kinase phosphorylation are all inhibited by the PI3 kinase inhibitor, LY 294002. The ligands for the EGFR/erbB1 receptor, EGF (epidermal growth factor) and TGF alpha (transforming growth factor- alpha ) demonstrate an increased ability to activate Akt in TAM-R compared with parental MCF-7 cells and it is proposed that the preferred autocrine or paracrine activation of Akt occurs via the erbB heterodimer EGFR/erbB2 in TAM-R cells. Akt phosphorylation is reduced by gefitinib ("Iressa"/ZD1839). The results suggest that the PI3 kinase pathway plays a role in proliferation of TAM-R cells and is important in the increased EGF induced membrane ruffling detected in the resistant cells. Increased Akt1 activation may contribute to the aggressive phenotype of tamoxifen resistant ER (oestrogen receptor) positive breast cancers.
他莫昔芬耐药(TAM-R)的MCF-7乳腺癌细胞系已被用作模型,以识别使耐药癌细胞能够独立于类固醇激素生长的信号通路。在TAM-R细胞中,肽生长因子信号通路似乎在细胞行为、生长和存活的改变中起重要作用。PI3激酶信号成分Akt1和Akt2在亲本野生型MCF-7细胞和TAM-R细胞中的表达水平相似,但在基础条件下生长的TAM-R细胞中,Akt1磷酸化显著增加。PI3激酶抑制剂LY 294002可抑制高水平的基础Akt、GSK3α/β和p70S6激酶磷酸化。与亲本MCF-7细胞相比,表皮生长因子受体(EGFR)/erbB1受体的配体表皮生长因子(EGF)和转化生长因子-α(TGFα)在TAM-R细胞中激活Akt的能力增强,并且有人提出,在TAM-R细胞中,Akt的优先自分泌或旁分泌激活是通过erbB异二聚体EGFR/erbB2发生的。吉非替尼(“易瑞沙”/ZD1839)可降低Akt磷酸化。结果表明,PI3激酶途径在TAM-R细胞的增殖中起作用,并且在耐药细胞中检测到的EGF诱导的膜皱襞增加中起重要作用。Akt1激活增加可能有助于他莫昔芬耐药的雌激素受体(ER)阳性乳腺癌的侵袭性表型。