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Beschreibung

A sulfonyldiphenylene-bis-dicyclohexylaminoacetamide compound that acts as a potent and selective inhibitor against adenovirus AVP, the cysteine proteinase critical for virion assembly and maturation, by targeting simultaneously AVP co-factor pVIc (GVQSLKRRRCF) N-terminal binding pocket (Ki = 150 nM) and AVP-pVIc substrate-binding site (Ki = 400 nM), blocking not only AVP-pVIc active complex formation/AVP activation (IC50 = 140 nM, [substrate] = 5 µ,M & [pVIc] = 40 µ,M), but also AVP-pVIc active complex catalytic activity (IC50 = 490 nM, [substrate] = 5 µ,M). Does not affect the activity of the serine protease trypsin or the cysteine protease papain even at concentrations as high as 10 µ,M., A sulfonyldiphenylene-bis-dicyclohexylaminoacetamide compound that acts as a potent and selective inhibitor against adenovirus cysteine proteinase AVP by targeting simultaneously AVP co-factor pVIc (GVQSLKRRRCF) N-terminal binding pocket (Ki = 150 nM) and AVP-pVIc substrate-binding site (Ki = 400 nM), blocking both AVP-pVIc active complex formation (IC50 = 140 nM, [substrate] = 5 µ,M & [pVIc] = 40 µ,M) and catalytic activity (IC50 = 490 nM, [substrate] = 5 µ,M) without affecting trypsin or papain protease activity even at concentrations as high as 10 µ,M.