Department 2 of Pharmaceutical Research, Chugai Pharmaceutical Co. Ltd, Kanagawa, Japan.
Cancer Sci. 2012 Dec;103(12):2144-52. doi: 10.1111/cas.12010. Epub 2012 Oct 30.
Lymphatic spread is an important clinical determinant in the prognosis of many human cancers. The lymphangiogenic factor vascular endothelial growth factor-D (VEGF-D) is implicated in the promotion of lymphatic metastasis through the development of lymphatic vessels in some human cancers. In this study, we developed an anti-VEGF-D monoclonal antibody, cVE199, and investigated its in vitro properties, in vivo effects against tumors and possible target indications to evaluate its potential as a therapeutic antibody. The cVE199 molecule was revealed to have a specific binding reactivity against human VEGF-D, as well as a specific inhibitory activity against the binding of human VEGF-D to VEGFR-3. In addition, cVE199 was found to inhibit the biological activity of VEGF-D against lymphatic cells in vitro. Because we determined that a neuroblastoma cell line, SK-N-DZ, abundantly expressed VEGF-D, an in vivo efficacy study was performed using a xenograft model of SK-N-DZ. We found that cVE199 significantly decreased lymphatic metastasis of SK-N-DZ as well as lymphangiogenesis in primary lesions. Finally, we investigated VEGF-D expression in human neuroblastoma, finding that the molecule was expressed in 11 of 29 human neuroblastoma specimens (37.9%). In conclusion, we found that a novel anti-VEGF-D monoclonal antibody, cVE199, with specific reactivity against human VEGF-D, prevents lymphatic metastasis of neuroblastoma through the inhibition of lymphangiogenesis in an animal model. In addition, our results show that VEGF-D is expressed in some cases of human neuroblastomas, which suggests that cVE199 is a potential anti-metastasis therapeutic antibody in neuroblastoma treatment.
淋巴扩散是许多人类癌症预后的重要临床决定因素。淋巴管生成因子血管内皮生长因子-D(VEGF-D)被认为通过在一些人类癌症中发展淋巴管促进淋巴转移。在这项研究中,我们开发了一种抗 VEGF-D 单克隆抗体 cVE199,并研究了其在体外的特性、对肿瘤的体内作用以及可能的靶标指示,以评估其作为治疗性抗体的潜力。cVE199 分子被揭示对人 VEGF-D 具有特异性结合反应性,以及对人 VEGF-D 与 VEGFR-3 结合的特异性抑制活性。此外,cVE199 被发现抑制 VEGF-D 在体外对淋巴细胞的生物学活性。因为我们确定神经母细胞瘤细胞系 SK-N-DZ 大量表达 VEGF-D,所以使用 SK-N-DZ 的异种移植模型进行了体内疗效研究。我们发现 cVE199 显著降低了 SK-N-DZ 的淋巴转移以及原发性病变中的淋巴管生成。最后,我们研究了人神经母细胞瘤中的 VEGF-D 表达,发现该分子在 29 个人神经母细胞瘤标本中的 11 个(37.9%)中表达。总之,我们发现一种新型抗 VEGF-D 单克隆抗体 cVE199 对人 VEGF-D 具有特异性反应性,可通过抑制动物模型中的淋巴管生成来预防神经母细胞瘤的淋巴转移。此外,我们的结果表明 VEGF-D 在一些人类神经母细胞瘤病例中表达,这表明 cVE199 是神经母细胞瘤治疗中潜在的抗转移治疗性抗体。