Zepatier: Difference between revisions

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== Structure and Mechanism of Grazoprevir ==

<scene name='74/745998/Grazoprevir/3'>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 C38H50N6O9S and has 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. For more interactive models of the Grazoprevir, click here [http://www.rcsb.org/pdb/explore/explore.do?structureId=5EPY]. 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. 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<ref>DOI: 10.1021/acschembio.5b00647</ref>.

<scene name='74/745998/Grazoprevir/3'>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 C38H50N6O9S and has 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 <scene name='74/746120/Catalytic_triad_of_ns3-4a/1'>catalytic triad</scene> of amino acids S139, H57 and D81, and an activating cofactor which assists in, and is required for the activity of the protease. For more interactive models of the Grazoprevir, click here [http://www.rcsb.org/pdb/explore/explore.do?structureId=5EPY]. 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. 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<ref>DOI: 10.1021/acschembio.5b00647</ref>.

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Revision as of 17:52, 4 December 2016 view source Megan Harris. (talk \| contribs) 72 edits No edit summary ← Older edit		Revision as of 18:43, 4 December 2016 view source Reafa Akhter Hossain (talk \| contribs) 16 edits No edit summary Newer edit →
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	== Structure and Mechanism of Grazoprevir ==		== Structure and Mechanism of Grazoprevir ==

	<scene name='74/745998/Grazoprevir/3'>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 has 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. For more interactive models of the Grazoprevir, click here [http://www.rcsb.org/pdb/explore/explore.do?structureId=5EPY]. 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. 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<ref>DOI: 10.1021/acschembio.5b00647</ref>.		<scene name='74/745998/Grazoprevir/3'>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 has 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 <scene name='74/746120/Catalytic_triad_of_ns3-4a/1'>catalytic triad</scene> of amino acids S139, H57 and D81, and an activating cofactor which assists in, and is required for the activity of the protease. For more interactive models of the Grazoprevir, click here [http://www.rcsb.org/pdb/explore/explore.do?structureId=5EPY]. 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. 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<ref>DOI: 10.1021/acschembio.5b00647</ref>.