Alexei Kisselev,Dmitry V. Filippov,Herman Overkleeft
申请号:
US13399189
公开号:
US08455431B2
申请日:
2012.02.17
申请国别(地区):
US
年份:
2013
代理人:
摘要:
The present invention is an inhibitor of the trypsin-like β2/β2i sites of the proteasome. The inhibitor is characterized as being a peptide-based epoxyketone or vinyl sulfone that contains an arginine or 4-aminomethylene-L-phenylalanine at the C-terminus (i.e., at the P1 position). Methods for using the inhibitor to inhibit the activity of the β2/β2i site of a proteasome and treat a proteasome-mediated disease or condition are also described.