1,2,3,4-tetrahydroacridin-9-amine |
inhibitor binding to Zn2+-free enzyme, dissociation constant 0.0017 mM, EC50 value 0.060 mM |
Hepacivirus C |
|
methyl [5-(thiophen-2-ylcarbonyl)-1H-benzimidazol-2-yl]carbamate |
inhibitor binding to Zn2+-free enzyme, dissociation constant 0.0019 mM, EC50 value 0.00003 mM |
Hepacivirus C |
|
additional information |
in the absence of Zn+2, the NS3 protease adopts a partially-folded inactive conformation. Identification of ligands binding to the Zn+2-free NS3 protease, that trap the inactive protein, and block the viral life cycle. Ligands show a new inhibition mechanism simultaneously blocking substrate and cofactor interactions in a non-competitive fashion, appropriate for combination therapy, low impact of known resistance-associated mutations and inhibition of NS4A binding, thus blocking its several effects on NS3 protease |
Hepacivirus C |
|