基本信息:
- 专利标题： REPROGRAMMING UROKINASE INTO AN ANTIBODY-RECRUITING ANTICANCER AGENT
- 专利标题（中）：将尿激酶转化成抗体受体反应剂
- 申请号：US14356820 申请日：2012-11-07
- 公开(公告)号：US20140308342A1 公开(公告)日：2014-10-16
- 发明人： David A. Spiegel , Charles E. Jakobsche
- 申请人： YALE UNIVERSITY
- 国际申请： PCT/US12/63844 WO 20121107
- 主分类号： C12N9/96
- IPC分类号： C12N9/96 ; C07K5/062 ; A61K38/05 ; A61K38/48 ; A61K45/06 ; C07D491/107 ; A61K31/352
摘要：
The present invention relates to chimeric (preferably, bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds preferably covalently bind to the urokinase receptor and recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and/or antibody-dependent cellular cytotoxicity (ADCC) against a large number and variety of cancers, thus providing cancer cell death and/or an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer.
摘要（中）：
本发明涉及嵌合（优选双官能）化合物，包含这些化合物的组合物和治疗患者或受试者中的癌症的方法，特别是包括转移性癌症，其中癌细胞表现出细胞表面尿激酶型纤溶酶原激活物受体的过表达（高表达） （尿激酶受体）与正常（非癌性）细胞相比。 化合物优选共价结合尿激酶受体并招募患者或受试者的天然抗体，其中抗体可以通过抗体依赖性细胞吞噬作用和/或抗体依赖性细胞毒性（ADCC）选择性降解和/或失活靶向癌细胞 大量和多种癌症，从而提供癌细胞死亡和/或抑制癌症的生长，修复和/或转移，包括缓解和治愈患者的癌症。