Targeting pancreatic cancer metastases with Targefrin

摘要 我们打算设计一种新的治疗策略，基于一种名为EphA2的特定癌细胞受体，该受体 在转移性胰腺癌表面大量存在。在过去的几年里，我们的研究集中在 检测靶向受体的药物在抑制细胞迁移和侵袭中的抗癌作用 细胞研究，以及使用体内模型抑制肿瘤转移。最近，我们推导出了 迄今为止报道的最有效的激动剂，它有效地靶向EphA2受体并导致其 退化。在初步研究中，该药物对抑制胰腺癌细胞非常有效 迁移。该制剂还导致受体内化；因此，我们打算探索我们是否可以 使用这种药物也可以选择性地将化疗输送到胰腺肿瘤。

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.