Institut für Pharmakologie, Universitätsklinikum Essen, Universität Duisburg-Essen, 45147 Essen, Germany.
J Biol Chem. 2010 Jul 23;285(30):23276-84. doi: 10.1074/jbc.M109.093146. Epub 2010 May 12.
Hyaluronan (HA) is a polysaccharide component in the parenchyma and stroma of human esophageal squamous cell carcinoma (ESCC). Clinically, esophageal cancer represents a highly aggressive tumor type with poor prognosis resulting in a 5-year survival rate of 5%. The aim of the present study was the detailed analysis of the role of HA synthesis for ESCC phenotype in vitro using the ESCC cell line OSC1. In OSC1 cells, pericellular HA-matrix surrounding extended actin-dependent filopodia was detected. The small molecule inhibitor of HA synthesis, 4-methylumbelliferone (4-MU, 0.3 mm) caused loss of these filopodia and focal adhesions and inhibited proliferation and migration. In search of the underlying mechanism cleavage of focal adhesion kinase (FAK) was detected by immunoblotting. In addition, displacing HA by an HA-binding peptide (Pep-1, 500 mug/ml) and digestion of pericellular HA by hyaluronidase resulted in cleavage of focal adhesions. Furthermore, real-time reverse transcription PCR revealed that HA synthase 3 (HAS3) > HAS2 are the predominant HA-synthases in OSC1. Lentiviral transduction with shHAS3, and to a lesser extent with shHAS2, reduced intact FAK protein and filopodia as well as proliferation and migration. Furthermore, down-regulation by lentiviral shRNA of RHAMM (receptor of HA-mediated motility) but not CD44 induced loss of filopodia and caused FAK cleavage. In contrast, knockdown of both HA receptors inhibited proliferation and migration of OSC1. In conclusion, HA synthesis and, in turn, RHAMM and CD44 signaling promoted an activated phenotype of OSC1. Because RHAMM appears to support both filopodia, FAK, and the proliferative and migratory phenotype, it may be promising to explore RHAMM as a potential therapeutic target in esophageal cancer.
透明质酸(HA)是人类食管鳞状细胞癌(ESCC)实质和基质中的多糖成分。临床上,食管癌是一种侵袭性很强的肿瘤类型,预后较差,5 年生存率为 5%。本研究的目的是使用 ESCC 细胞系 OSC1 详细分析 HA 合成对 ESCC 表型的体外作用。在 OSC1 细胞中,检测到围绕延伸的肌动蛋白依赖性丝状伪足的细胞周 HA 基质。HA 合成的小分子抑制剂 4-甲基伞形酮(4-MU,0.3mm)导致这些丝状伪足和焦点粘连的丢失,并抑制增殖和迁移。为了寻找潜在的机制,通过免疫印迹检测到粘着斑激酶(FAK)的裂解。此外,通过 HA 结合肽(Pep-1,500μg/ml)置换 HA 和通过透明质酸酶消化细胞周 HA 导致焦点粘连的裂解。此外,实时逆转录 PCR 显示 HA 合酶 3(HAS3)>HAS2 是 OSC1 中主要的 HA 合酶。用慢病毒转导 shHAS3,在较小程度上用 shHAS2,减少完整的 FAK 蛋白和丝状伪足以及增殖和迁移。此外,慢病毒 shRNA 下调 RHAMM(HA 介导的运动受体)而不是 CD44 导致丝状伪足丢失并引起 FAK 裂解。相反,HA 受体的敲低均抑制 OSC1 的增殖和迁移。总之,HA 合成,继而 RHAMM 和 CD44 信号促进了 OSC1 的激活表型。因为 RHAMM 似乎支持丝状伪足、FAK 和增殖和迁移表型,因此探索 RHAMM 作为食管癌的潜在治疗靶点可能是有希望的。