Matthew S. Bogyo,Galia Blum,Alicia Berger,Zhen Cheng,Sanjiv S. Gambhir
申请号：
US12418116
公开号：
US08343458B2
申请日:
2009.04.03
申请国别(地区):
US
年份:
2013
代理人:
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.
