发明申请
- 专利标题: Probes for In Vivo Targeting of Active Cysteine Proteases
- 专利标题(中): 体内靶向活性半胱氨酸蛋白酶的探针
-
申请号: US12418116申请日: 2009-04-03
-
公开(公告)号: US20090252677A1公开(公告)日: 2009-10-08
- 发明人: Matthew S. Bogyo , Galia Blum , Alicia Berger , Zhen Cheng , Sanjiv S. Gambhir
- 申请人: Matthew S. Bogyo , Galia Blum , Alicia Berger , Zhen Cheng , Sanjiv S. Gambhir
- 申请人地址: US CA Palo Alto
- 专利权人: The Board of Trustees of the Leland Stanford Junior University
- 当前专利权人: The Board of Trustees of the Leland Stanford Junior University
- 当前专利权人地址: US CA Palo Alto
- 主分类号: A61K51/04
- IPC分类号: A61K51/04 ; A61K49/00 ; A61P35/00
摘要:
Activity-based probes, which are specific for certain active cysteine proteases (caspase, cathepsin and legumain) and carry radioactive labels, are disclosed. The present probes comprise an acyloxymethyketone (AOMK) “warhead” that binds only to active enzyme. The probes further comprise peptide-like structure that targets the probe to a specific cysteine protease or protease family, and a radiolabel on the probe, which is bound to the targeted enzyme. It has been found that the present probes are stable in vivo and give specific target images distinguishable over background. The preferred probes are labeled with a positron-emitting agent such as 64Cu, 125I (SPECT) and 99mTc (PET). The probes show in vivo half-life and stability well suited for imaging.
公开/授权文献
- US08343458B2 Probes for in vivo targeting of active cysteine proteases 公开/授权日:2013-01-01
信息查询