Laboratory of Molecular Targeted Therapy of Cancer, Institute of Basic Medical Sciences, Hubei University of Medicine, Shiyan, China.
Hubei Key Laboratory of Wudang Local Chinese Medicine Research, Hubei University of Medicine, Shiyan, China.
Cancer Sci. 2021 Dec;112(12):4867-4882. doi: 10.1111/cas.15151. Epub 2021 Oct 20.
G protein pathway suppressor 2 (GPS2) is expressed in most human tissues, including the stomach. However, the biological functions of GPS2 in cancer, as well as the underlying molecular mechanisms, remain poorly understood. Here, we report that GPS2 expression was aberrantly downregulated in gastric cancer (GC) tissues compared with control tissues. Clinicopathologic analysis showed that low GPS2 expression was significantly correlated with pathological grade, lymph node stage, and invasive depth. Kaplan-Meier analysis indicated that patients with low GPS2 expression showed poorer overall survival rates than those with high GPS2 expression. Moreover, GPS2 overexpression decreased GC cell proliferation, colony formation, tumorigenesis, and invasion. Overexpression of GPS2 reduced the protein expression of epidermal growth factor receptor (EGFR) and inhibited its downstream signaling in GC cells. Interestingly, GPS2 decreased EGFR protein expression, which was reversed by a lysosome inhibitor. Furthermore, GPS2 reduced EGFR protein stability by enhancing the binding of EGFR and an E3 ligase, c-Cbl, which promoted the ubiquitination of EGFR, ultimately leading to its degradation through the lysosomal pathway. Further analysis indicated that GPS2 activated autophagy and promoted the autophagic flux by destabilizing EGFR. Taken together, these results suggest that low GPS2 expression is associated with GC progression and provide insights into the applicability of the GPS2-EGFR axis as a potential therapeutic target in GC.
G 蛋白通路抑制因子 2(GPS2)在大多数人体组织中表达,包括胃。然而,GPS2 在癌症中的生物学功能以及潜在的分子机制仍知之甚少。在这里,我们报告 GPS2 在胃癌(GC)组织中的表达与对照组织相比异常下调。临床病理分析表明,GPS2 低表达与病理分级、淋巴结分期和浸润深度显著相关。Kaplan-Meier 分析表明,GPS2 低表达的患者总生存率低于 GPS2 高表达的患者。此外,GPS2 的过表达降低了 GC 细胞的增殖、集落形成、肿瘤发生和侵袭。在 GC 细胞中过表达 GPS2 降低了表皮生长因子受体(EGFR)的蛋白表达,并抑制了其下游信号通路。有趣的是,GPS2 降低 EGFR 蛋白表达,这可以被溶酶体抑制剂逆转。此外,GPS2 通过增强 EGFR 和 E3 连接酶 c-Cbl 的结合来降低 EGFR 蛋白稳定性,从而促进 EGFR 的泛素化,最终通过溶酶体途径导致其降解。进一步分析表明,GPS2 通过不稳定 EGFR 激活自噬并促进自噬通量。综上所述,这些结果表明 GPS2 低表达与 GC 进展有关,并为 GPS2-EGFR 轴作为 GC 潜在治疗靶点的适用性提供了新的见解。