Departamento de Química Biológica, Facultad de Farmacia y Bioquímica, Instituto de Química y Fisicoquímica Biológicas (UBA-CONICET), Universidad de Buenos Aires, Buenos Aires, Argentina.
J Endocrinol. 2010 Mar;204(3):299-309. doi: 10.1677/JOE-09-0372. Epub 2009 Dec 23.
Epidermal growth factor (EGF) is a key regulator of cell survival and proliferation involved in the pathogenesis and progression of different types of cancer. The EGF receptor (EGFR) is activated by binding of the specific ligand but also by transactivation triggered by different growth factors including GH. Chronically, elevated GH levels have been associated with the progression of hepatocellular carcinoma. Considering EGF and GH involvement in cell proliferation and their signaling crosstalk, the objective of the present study was to analyze GH modulatory effects on EGF signaling in liver. For this purpose, GH receptor-knockout (GHR-KO) and GH-overexpressing transgenic mice were used. EGFR content was significantly decreased in GHR-KO mice. Consequently, EGF-induced phosphorylation of EGFR, AKT, ERK1/2, STAT3, and STAT5 was significantly decreased in these mice. In contrast, EGFR content as well as its basal tyrosine phosphorylation was increased in transgenic mice overexpressing GH. However, EGF stimulation caused similar levels of EGFR, AKT, and ERK1/2 phosphorylation in normal and transgenic mice, while EGF induction of STAT3 and STAT5 phosphorylation was inhibited in the transgenic mice. Desensitization of the STATs was related to decreased association of these proteins to the EGFR and increased association between STAT5 and the tyrosine phosphatase SH2-containing phosphatase-2. While GHR knockout is associated with diminished expression of the EGFR and a concomitant decrease in EGF signaling, GH overexpression results in EGFR overexpression with different effects depending on the signaling pathway analyzed: AKT and ERK1/2 pathways are induced by EGF, while STAT3 and STAT5 activation is heterologously desensitized.
表皮生长因子(EGF)是一种细胞存活和增殖的关键调节因子,参与不同类型癌症的发病机制和进展。EGF 受体(EGFR)通过特定配体的结合而被激活,但也通过包括 GH 在内的不同生长因子的转激活而被激活。长期以来,升高的 GH 水平与肝细胞癌的进展有关。考虑到 EGF 和 GH 参与细胞增殖及其信号转导的串扰,本研究的目的是分析 GH 对肝脏中 EGF 信号的调节作用。为此,使用了 GH 受体敲除(GHR-KO)和 GH 过表达转基因小鼠。GHR-KO 小鼠的 EGFR 含量显著降低。因此,在这些小鼠中,EGF 诱导的 EGFR、AKT、ERK1/2、STAT3 和 STAT5 的磷酸化显著降低。相比之下,在过表达 GH 的转基因小鼠中,EGFR 含量及其基础酪氨酸磷酸化增加。然而,EGF 刺激在正常和转基因小鼠中引起类似水平的 EGFR、AKT 和 ERK1/2 磷酸化,而 EGF 诱导的 STAT3 和 STAT5 磷酸化在转基因小鼠中受到抑制。STATs 的脱敏与这些蛋白与 EGFR 的结合减少以及 STAT5 与含 SH2 的磷酸酶-2 之间的酪氨酸磷酸酶结合增加有关。虽然 GHR 敲除与 EGFR 的表达减少和 EGF 信号的相应减少有关,但 GH 过表达导致 EGFR 过表达,其对不同信号通路的影响取决于所分析的信号通路:AKT 和 ERK1/2 通路被 EGF 诱导,而 STAT3 和 STAT5 的激活被异源脱敏。