Huib Ovaa,Reggy Ekkebus,Sander Izaäk Van Kasteren,Annemieke De Jong,Paulus Petrus Geurink
申请号：
US14412990
公开号：
US20150158931A1
申请日:
2013.07.05
申请国别(地区):
US
年份:
2015
代理人:
摘要：
The invention concerns cysteine protease capturing agents capable of highly selective and irreversible binding of the corresponding cysteine protease. Such compounds may have utility in fundamental biological research and diagnostics, e.g. involving labeled or immobilized versions of such compounds, and they may also have potential utility in therapy, based on competitive inhibition of the cysteine protease, as will be readily apparent to those skilled in the art. The present inventors have discovered that such capturing agents can be obtained by modification of a cleavage fragment of a ‘natural’ substrate for the cysteine protease of interest, said modification involving the introduction of a propargyl moiety in such a way that the terminal alkyne group is positioned to allow for interaction with the free thiol group of the cysteine residue at the active site of the protease.
