hcv ns3/4a protease

Glecaprevir (ABT-493) is an HCV NS3 4A protease inhibitor, (IC50s: 3.5-11.3 nM).

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.

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.

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.

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

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

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

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

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.

Paritaprevir (ABT450) is an inhibitor of non-structural protein 3 4A protease with EC50 values of 1 and 0.21 nM for HCV 1a and HCV 1b, respectively.

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

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.

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

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. NS3, a serine protease, is essential for the proteolytic cleavage of multiple sites within the HCV polyprotein and plays a key role during HCV ribonucleic acid (RNA) replication. NS4A is an activating factor for NS3. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family, and infection is associated with the development of hepatocellular carcinoma (HCC).

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

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].

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