hcv ns3/4a protease

HZ-1157 (DHFR-inhibitor) is a hepatitis C virus (HCV) inhibitor with inhibitory activities toward HCV NS3/4A protease.

Asunaprevir (BMS-650032) is an effective hepatitis C virus (HCV) NS3 protease inhibitor.

Grazoprevir (MK-5172) is a nitrogenous macrocyclic compound used as an inhibitor of the hepatitis C virus NS3/4A protease. Grazoprevir is commonly combined with elbasvir for treating chronic HCV genotype 1 or 4 infections in adults.

Simeprevir (TMC435) is a potent HCV NS3/4A protease inhibitor, and inhibits HCV replication with EC50 of 8 nM.

Glecaprevir (ABT-493) is a small-molecule inhibitor that functions as an HCV NS3/4A protease inhibitor (IC50=3.5–11.3 nM) and also inhibits SARS-CoV-2 3CLpro (IC50=4.09 μM). It possesses oral bioavailability and antiviral activity, and is used for the treatment of hepatitis C as well as potential anti-coronavirus research.

Danoprevir (RG7227) is a peptidomimetic inhibitor of the NS3/4A protease(IC50=0.2-3.5 nM) of hepatitis C virus (HCV).

4-Phenoxybenzylamine inhibits the function of the NS3 protein by stabilizing an inactive conformation, with an IC50 of approximately 500 μM against HCV NS3/4a.

Faldaprevir is an orally effective, selective, non-covalent HCV NS3/4A protease inhibitor with high inhibitory activity against HCV 1a and 1b genotypes (Ki=2.6 nM &2.0 nM).Faldaprevir inhibits viral replication by blocking the breakdown of viral precursor proteins, and is well tolerated with good antiviral activity against hepatitis C virus.

Vaniprevir is a non-covalent competitive HCV NS3/4A protease inhibitor, an antiviral drug that acts directly on the hepatitis C virus. Vaniprevir blocks the viral replication process by inhibiting the activity of HCV NS3/4A protease.

Voxilaprevir is an inhibitor of hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease.

MK-6325 is a potent inhibitor of the HCV NS3/4A protease.

Paritaprevir free base (ABT-450) is an orally bioavailable, synthetic acylsulfonamide inhibitor of the hepatitis C virus (HCV) protease complex comprised of non-structural protein 3 and 4A (NS3/NS4A), with potential activity against HCV genotype 1. Upon administration, paritaprevir reversibly binds to the active center and binding site of the HCV NS3/NS4A protease and prevents NS3/NS4A protease-mediated polyprotein maturation. This disrupts both the processing of viral proteins and the formation of the viral replication complex, which inhibits viral replication in HCV genotype 1-infected host cells.

Telaprevir (Incivek) (VX-950) is an effective inhibitor of HCV NS3-4A serine protease (IC50: 0.35 μM).

Paritaprevir dihydrate (ABT-450), a highly effective and orally administered antiviral, acts as a non-structural protein 3/4A (NS3/4A) protease inhibitor, displaying EC50 values of 1 and 0.21 nM against HCV genotypes 1a and 1b, respectively. Additionally, it functions as a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Primarily metabolized by cytochrome P450 (CYP) 3A, its plasma concentration and half-life are significantly increased when administered with Ritonavir, a CYP450 inhibitor [1] [2] [3] [4].

Variculanol, a compound with antimicrobial, anticancer, and anti-HCV NS3/4A protease properties, is derived from the marine fungus Aspergillus versicolor [1].

KK4A peptide, a small peptide derived from the nonstructural protein 4A (NS4A) of Hepatitis C virus (HCV), significantly enhances the catalytic efficiency of the NS3 protease. This peptide serves as a valuable tool for further understanding the function and mechanism of the HCV NS3 protease, thereby advancing research on HCV infections.