Department of Cancer Biology, Mayo Clinic College of Medicine, Jacksonville, Florida 32224, USA.
Cancer Res. 2010 Mar 1;70(5):2064-74. doi: 10.1158/0008-5472.CAN-09-2684. Epub 2010 Feb 23.
Pancreatic cancer is the fourth leading cause of cancer deaths in the United States, with an overall 5-year survival rate of <5%. Pancreatic ductal adenocarcinoma (PDAC), the most common form of pancreatic cancer, is highly resistant to conventional chemotherapies, underscoring the critical need for new molecular targets for pancreatic cancer chemotherapy. The KRAS proto-oncogene is mutated in >90% of PDAC. Protein kinase Ciota (PKCiota) is required for the oncogenic Ras-mediated transformed growth of lung cancer and intestinal epithelial cells. However, little is known about the role of PKCiota in pancreatic cancer. In this study, we evaluated the expression of PKCiota in human pancreatic cancer and the requirement for PKCiota for the transformed growth and tumorigenicity of PDAC cells. We find that PKCiota is significantly overexpressed in human pancreatic cancer, and high PKCiota expression correlates with poor patient survival. Inhibition of PKCiota expression blocks PDAC cell transformed growth in vitro and tumorigenicity in vivo. Inhibition of PKCiota expression in pancreatic tumors also significantly reduces tumor angiogenesis and metastasis. Analysis of downstream PKCiota effectors implicates the Rac1-MEK/ERK1/2 signaling axis in PKCiota-mediated transformed growth and cellular invasion. Taken together, our data show a required role for PKCiota in the transformed growth of pancreatic cancer cells and reveal a novel role for PKCiota in pancreatic cancer cell metastasis and angiogenesis in vivo. Our results strongly indicate that PKCiota will be an effective target for pancreatic cancer therapy.
胰腺癌是美国第四大癌症死亡原因,总体 5 年生存率<5%。胰腺导管腺癌(PDAC)是最常见的胰腺癌形式,对传统化疗具有高度耐药性,这突显了寻找新的胰腺癌化疗分子靶点的迫切需要。KRAS 原癌基因在>90%的 PDAC 中发生突变。蛋白激酶 Ciota(PKCiota)是肺癌和肠上皮细胞中致癌 Ras 介导的转化生长所必需的。然而,PKCiota 在胰腺癌中的作用知之甚少。在这项研究中,我们评估了 PKCiota 在人胰腺癌中的表达以及 PKCiota 对 PDAC 细胞转化生长和致瘤性的要求。我们发现 PKCiota 在人胰腺癌中显著过表达,高 PKCiota 表达与患者预后不良相关。抑制 PKCiota 表达可阻断 PDAC 细胞体外转化生长和体内致瘤性。在胰腺肿瘤中抑制 PKCiota 表达也显著减少肿瘤血管生成和转移。对 PKCiota 下游效应器的分析表明,Rac1-MEK/ERK1/2 信号通路参与了 PKCiota 介导的转化生长和细胞侵袭。总之,我们的数据表明 PKCiota 在胰腺癌细胞的转化生长中起着必需的作用,并揭示了 PKCiota 在胰腺癌细胞转移和体内血管生成中的新作用。我们的结果强烈表明,PKCiota 将成为胰腺癌治疗的有效靶点。