Institute of Cancer Stem Cell, Dalian Medical University, Dalian, 116044, China.
Department of Physiology, College of Basic Medical Sciences, Dalian Medical University, Dalian, 116044, China.
J Exp Clin Cancer Res. 2018 Jul 28;37(1):176. doi: 10.1186/s13046-018-0842-z.
Adaptation to ER stress has been indicated to play an important role in resistance to therapy in human melanoma. However, the relationship between adaptation to ER stress and cell metastasis in human melanoma remains unclear.
The relationship of adaptation to ER stress and cell metastasis was investigated using transwell and mouse metastasis assays. The potential molecular mechanism of KLF4 in regulating the adaptation to ER stress and cell metastasis was investigated using RNA sequencing analysis, q-RT-PCR and western blot assays. The transcriptional regulation of nucleobindin 2 (NUCB2) by KLF4 was identified using bioinformatic analysis, luciferase assay, and chromatin immunoprecipitation (ChIP). The clinical significance of KLF4 and NUCB2 was based on human tissue microarray (TMA) analysis.
Here, we demonstrated that KLF4 was induced by ER stress in melanoma cells, and increased KLF4 inhibited cell apoptosis and promoted cell metastasis. Further mechanistic studies revealed that KLF4 directly bound to the promoter of NUCB2, facilitating its transcription. Additionally, an increase in KLF4 promoted melanoma ER stress resistance, tumour growth and cell metastasis by regulating NCUB2 expression in vitro and in vivo. Elevated KLF4 was found in human melanoma tissues, which was associated with NUCB2 expression.
Our data revealed that the promotion of ER stress resistance via the KLF4-NUCB2 axis is essential for melanoma cell metastasis, and KLF4 may be a promising specific target for melanoma therapy.
内质网应激适应被认为在人类黑色素瘤的治疗耐药中起重要作用。然而,内质网应激适应与人类黑色素瘤细胞转移之间的关系尚不清楚。
使用 Transwell 和小鼠转移实验研究内质网应激适应与细胞转移之间的关系。使用 RNA 测序分析、q-RT-PCR 和 Western blot 分析研究 KLF4 调节内质网应激适应和细胞转移的潜在分子机制。使用生物信息学分析、荧光素酶测定和染色质免疫沉淀(ChIP)鉴定 KLF4 对核结合蛋白 2(NUCB2)的转录调控。基于人类组织微阵列(TMA)分析研究 KLF4 和 NUCB2 的临床意义。
我们证明了 KLF4 在黑色素瘤细胞中被内质网应激诱导,增加的 KLF4 抑制细胞凋亡并促进细胞转移。进一步的机制研究表明,KLF4 直接结合到 NUCB2 的启动子上,促进其转录。此外,KLF4 的增加通过调节体外和体内的 NCUB2 表达促进了黑色素瘤的内质网应激抵抗、肿瘤生长和细胞转移。在人类黑色素瘤组织中发现 KLF4 升高,与 NUCB2 表达相关。
我们的数据揭示了通过 KLF4-NUCB2 轴促进内质网应激适应对于黑色素瘤细胞转移是至关重要的,并且 KLF4 可能是黑色素瘤治疗的有前途的特异性靶标。