Targeting pancreatic cancer metastases with Targefrin

摘要 我们打算设计一种基于名为EphA 2的特异性癌细胞受体的新型治疗策略， 在转移性胰腺癌的表面大量存在在过去的几年里，我们的研究集中在 测试靶向受体的药剂在抑制细胞迁移和侵袭中的抗癌潜力， 细胞研究以及使用体内模型抑制肿瘤转移。最近我们得到了 迄今为止报道的最有效的激动剂，其有效靶向EphA 2受体并引起其 降解在初步研究中，该试剂对抑制胰腺癌细胞有显著效果， 迁移该试剂也引起受体的内化;因此，我们打算探索我们是否可以 也可以使用这种药物选择性地对胰腺肿瘤进行化疗。

ABSTRACT We intend to devise a novel therapeutic strategy based on a specific cancer cell receptor named EphA2, which is abundant on the surface of metastatic pancreatic cancers. Over the past several years our studies focused on testing the anti-cancer potential of agents targeting the receptor in suppressing cell migration and invasion in cellular studies, as well as in inhibiting tumor metastases using in vivo models. Very recently we have derived the most effective agonistic agent reported to date that potently targets the EphA2 receptor and causes its degradation. In preliminary studies, the agent is remarkably effective in inhibiting pancreatic cancer cell migration. The agent also causes the internalization of the receptor; hence we intend to probe whether we can use this agent also to deliver chemotherapy selectively to pancreatic tumors.