HER4的胞质结构域而非其C末端可抑制乳腺细胞增殖。

The HER4 cytoplasmic domain, but not its C terminus, inhibits mammary cell proliferation.

作者信息

Feng Shu-Mang, Sartor Carolyn I, Hunter Debra, Zhou Hong, Yang Xihui, Caskey Laura S, Dy Ruth, Muraoka-Cook Rebecca S, Earp H Shelton

机构信息

University of North Carolina Chapel Hill, Lineberger Comprehensive Cancer Center, Chapel Hill, North Carolina 27599, USA.

出版信息

Mol Endocrinol. 2007 Aug;21(8):1861-76. doi: 10.1210/me.2006-0101. Epub 2007 May 15.

Abstract

Unlike the proliferative action of other epidermal growth factor (EGF) receptor family members, HER4/ErbB4 is often associated with growth-inhibitory and differentiation signaling. These actions may involve HER4 two-step proteolytic processing by intramembraneous gamma-secretase, releasing the soluble, intracellular 80-kDa HER4 cytoplasmic domain, s80HER4. We demonstrate that pharmacological inhibition of either gamma-secretase activity or HER4 tyrosine kinase activity blocked heregulin-dependent growth inhibition of SUM44 breast cancer cells. We next generated breast cell lines stably expressing GFP-s80HER4 [green fluorescent protein (GFP) fused to the N terminus of the HER4 cytoplasmic domain, residues 676-1308], GFP-CT(HER4) (GFP fused to N terminus of the HER4 C-terminus distal to the tyrosine kinase domain, residues 989-1308), or GFP alone. Both GFP-s80HER4 and GFP-CTHER4 were found in the nucleus, but GFP-s80HER4 accumulated to a greater extent and sustained its nuclear localization. s80HER4 was constitutively tyrosine phosphorylated, and treatment of cells with a specific HER family tyrosine kinase inhibitor 1) blocked tyrosine phosphorylation; 2) markedly diminished GFP-s80HER4 nuclear localization; and 3) reduced signal transducer and activator of transcription (STAT)5A tyrosine phosphorylation and nuclear localization as well as GFP-s80HER4:STAT5A interaction. Multiple normal mammary and breast cancer cell lines, stably expressing GFP-s80HER4 (SUM44, MDA-MB-453, MCF10A, SUM102, and HC11) were growth inhibited compared with the same cell line expressing GFP-CTHER4 or GFP alone. The s80HER4-induced cell number reduction was due to slower growth because rates of apoptosis were equivalent in GFP-, GFP-CTHER4-, and GFP-s80HER4-expressing cells. Lastly, GFP-s80HER4 enhanced differentiation signaling as indicated by increased basal and prolactin-dependent beta-casein expression. These results indicate that surface HER4 tyrosine phosphorylation and ligand-dependent release of s80HER4 are necessary, and s80HER4 signaling is sufficient for HER4-dependent growth inhibition.

摘要

与其他表皮生长因子(EGF)受体家族成员的增殖作用不同,HER4/ErbB4通常与生长抑制和分化信号相关。这些作用可能涉及HER4经膜内γ-分泌酶进行的两步蛋白水解过程,释放出可溶性的细胞内80 kDa HER4胞质结构域,即s80HER4。我们证明,对γ-分泌酶活性或HER4酪氨酸激酶活性的药理学抑制可阻断这里调节蛋白依赖性的SUM44乳腺癌细胞生长抑制。接下来,我们构建了稳定表达GFP-s80HER4[绿色荧光蛋白(GFP)与HER4胞质结构域的N端融合,氨基酸残基676 - 1308]、GFP-CT(HER4)(GFP与HER4酪氨酸激酶结构域远端的C端N端融合,氨基酸残基989 - 1308)或单独GFP的乳腺细胞系。发现GFP-s80HER4和GFP-CTHER4均存在于细胞核中,但GFP-s80HER4积累程度更高且维持其核定位。s80HER4持续发生酪氨酸磷酸化,用特异性HER家族酪氨酸激酶抑制剂处理细胞:1)阻断酪氨酸磷酸化;2)显著减少GFP-s80HER4的核定位;3)降低信号转导和转录激活因子(STAT)5A的酪氨酸磷酸化和核定位以及GFP-s80HER4:STAT5A相互作用。与表达GFP-CTHER4或单独GFP的相同细胞系相比,稳定表达GFP-s80HER4的多种正常乳腺和乳腺癌细胞系(SUM44、MDA-MB-453、MCF10A、SUM102和HC11)生长受到抑制。s80HER4诱导的细胞数量减少是由于生长较慢,因为在表达GFP、GFP-CTHER4和GFP-s80HER4的细胞中凋亡率相当。最后,如基础和催乳素依赖性β-酪蛋白表达增加所示,GFP-s80HER4增强了分化信号。这些结果表明,表面HER4酪氨酸磷酸化和s80HER4的配体依赖性释放是必要的,并且s80HER4信号足以实现HER4依赖性的生长抑制。

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