Institute of Digestive Disease and Department of Medicine and Therapeutics, State Key Laboratory of Digestive Disease, Li Ka Shing Institute of Health Sciences, The Chinese University of Hong Kong, Hong Kong, China.
Department of Surgery, Hebei Medical University 4th Hospital, Shijiazhuang, China.
Oncogene. 2021 May;40(19):3422-3433. doi: 10.1038/s41388-021-01656-1. Epub 2021 Apr 21.
Peritoneal metastasis is a common form of metastasis among advanced gastric cancer patients. In this study, we reported the identification of LIM domain kinase 1 (LIMK1) as a promoter of gastric cancer peritoneal metastasis, and its potential to be a therapeutic target of dabrafenib (DAB). Using transcriptomic sequencing of paired gastric cancer peritoneal metastasis, primary tumors, and normal gastric tissues, we first unveiled that LIMK1 is selectively up-regulated in metastatic tumors. Increased LIMK1 in gastric cancer peritoneal metastasis was validated by immunohistochemistry analysis of an independent patient cohort. In vitro functional studies demonstrated that LIMK1 knockout or knockdown significantly inhibited cell migration and invasion of gastric cancer cells. LIMK1 knockout also abrogated peritoneal and liver metastases of gastric cancer cells in nude mice in vivo. Dabrafenib, a small molecule targeting LIMK1, was found to decrease cell migration and invasion of gastric cancer cells in vitro and abolish peritoneal and liver metastasis formation in vivo. Mechanistically, either LIMK1 knockout or Dabrafenib inhibited LIMK1 expression and phosphorylation of its downstream target cofilin. Taken together, our results demonstrated that LIMK1 functions as a metastasis promoter in gastric cancer by inhibiting LIMK1-p-cofilin and that Dabrafenib has the potential to serve as a novel treatment for gastric cancer peritoneal metastasis.
腹膜转移是晚期胃癌患者常见的转移形式。在本研究中,我们发现 LIM 结构域激酶 1(LIMK1)是促进胃癌腹膜转移的一个关键分子,并证实其可能成为达拉非尼(DAB)的治疗靶点。我们通过对配对的胃癌腹膜转移灶、原发灶和正常胃组织进行转录组测序,首次揭示 LIMK1 在转移性肿瘤中选择性地上调。通过对独立的患者队列进行免疫组织化学分析,验证了胃癌腹膜转移中 LIMK1 的增加。体外功能研究表明,LIMK1 敲除或敲低显著抑制了胃癌细胞的迁移和侵袭。LIMK1 敲除还消除了裸鼠体内胃癌细胞的腹膜和肝转移。靶向 LIMK1 的小分子达拉非尼被发现可减少体外胃癌细胞的迁移和侵袭,并在体内消除腹膜和肝转移的形成。从机制上讲,LIMK1 敲除或达拉非尼抑制了 LIMK1 及其下游靶蛋白丝切蛋白的表达和磷酸化。综上所述,我们的研究结果表明,LIMK1 通过抑制 LIMK1-p-cofilin 在胃癌中发挥转移促进作用,达拉非尼有可能成为治疗胃癌腹膜转移的新方法。