User:Megan Harris./Sandbox 1: Difference between revisions

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Zepatier is a combination drug combating genotypes 1 and 4 of chronic hepatitis C viral (HCV) infections in adults. <scene name='74/745998/Elbasvir_structure1/1'>Elbasvir</scene> inhibits NS5A, a non-enzymatic protein essential for viral replication and assembly of hepatitis C whose exact mechanism of action is unknown. Elbasvir prevents viral production at the early stage of assembly in turn preventing spread of the virus.  
Zepatier is a combination drug combating genotypes 1 and 4 of chronic hepatitis C viral (HCV) infections in adults. <scene name='74/745998/Elbasvir_structure1/1'>Elbasvir</scene> inhibits NS5A, a non-enzymatic protein essential for viral replication and assembly of hepatitis C whose exact mechanism of action is unknown. Elbasvir prevents viral production at the early stage of assembly in turn preventing spread of the virus.  
<scene name='74/745998/Grazoprevir_structure/1'>Grazoprevir</scene> is a macrocyclic compound that is able to reversibly bind to the protease, NS3/4A. NS3/4A is a serine protease also essential for viral replication. It is responsible for cleavage and processing of the HCV polyprotein. It is hypothesized that the protease is utilized to circumvent immune response at the primary stages of infection <ref>DOI: 10.1021/acschembio.5b00647</ref>.
Grazoprevir is a macrocyclic compound that is able to reversibly bind to the protease, NS3/4A. NS3/4A is a serine protease also essential for viral replication. It is responsible for cleavage and processing of the HCV polyprotein. It is hypothesized that the protease is utilized to circumvent immune response at the primary stages of infection <ref>DOI: 10.1021/acschembio.5b00647</ref>.




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== Mechanism of Grazoprevir ==  
== Mechanism of Grazoprevir ==  


<scene name='74/745998/Grazoprevir_structure/1'>Grazoprevir</scene> stops the hepatitis C virus by inhibiting the NS3/4A protease, which is an enzyme responsible for the cleavage of the viral polyprotein. The molecular formula is C<sub>38</sub>H<sub>50</sub>N<sub>6</sub>O<sub>9</sub>S and a molecular weight of 766.911 g/mol <ref>National Center for Biotechnology Information. PubChem Compound Database; CID=44603531, https://pubchem.ncbi.nlm.nih.gov/compound/44603531.</ref>. Cleavage of this polyprotein facilitates viral assembly and maturation of the virus. The NS3/4A protease is a protein complex in which the active site consists of a catalytic triad of amino acids S139, H57 and D81, and an activating cofactor which assists in, and is required for the activity of the protease. Grazoprevir has been proven to be more effective than similar protease inhibitors due to its two-way approach to inhibition. NS3/4A protease cleaves both the viral polyprotein of the Hep C virus and host factors involved in the immune response, such as TRIF and MAVS. Grazoprevir is unique in regard to its P4 cap, and P2 to P4 macrocyclic restriction, which interacts with the catalytic triad of the NS3/4A protease in its own distinct conformation. In this conformation, the P2 region is comprised of the Histidine-57 and Aspartate-81 residues.
Grazoprevir stops the hepatitis C virus by inhibiting the NS3/4A protease, which is an enzyme responsible for the cleavage of the viral polyprotein. The molecular formula is C<sub>38</sub>H<sub>50</sub>N<sub>6</sub>O<sub>9</sub>S and a molecular weight of 766.911 g/mol <ref>National Center for Biotechnology Information. PubChem Compound Database; CID=44603531, https://pubchem.ncbi.nlm.nih.gov/compound/44603531.</ref>. Cleavage of this polyprotein facilitates viral assembly and maturation of the virus. The NS3/4A protease is a protein complex in which the active site consists of a catalytic triad of amino acids S139, H57 and D81, and an activating cofactor which assists in, and is required for the activity of the protease. Grazoprevir has been proven to be more effective than similar protease inhibitors due to its two-way approach to inhibition. NS3/4A protease cleaves both the viral polyprotein of the Hep C virus and host factors involved in the immune response, such as TRIF and MAVS. Grazoprevir is unique in regard to its P4 cap, and P2 to P4 macrocyclic restriction, which interacts with the catalytic triad of the NS3/4A protease in its own distinct conformation. In this conformation, the P2 region is comprised of the Histidine-57 and Aspartate-81 residues.


== Disease ==
== Disease ==
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