Zepatier: Difference between revisions

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== Structure and Mechanism of Grazoprevir ==

<scene name='74/745998/Grazoprevir/3'>Grazoprevir</scene> (C38H50N6O9, molecular weight: 766.911 g/mol) <ref>National Center for Biotechnology Information. PubChem Compound Database; CID=44603531, https://pubchem.ncbi.nlm.nih.gov/compound/44603531.</ref> stops the hepatitis C virus by inhibiting the NS3/4A protease, which is an enzyme responsible for the cleavage of the viral polyprotein. 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. Due to this conformation, Grazoprevir can easily bind to the catalytic triad because it is already in a highly favorable arrangement, stopping the triads activity.<ref>DOI: 10.1021/acschembio.5b00647</ref>.

<scene name='74/745998/Grazoprevir/3'>Grazoprevir</scene> (C38H50N6O9, molecular weight: 766.911 g/mol) <ref>National Center for Biotechnology Information. PubChem Compound Database; CID=44603531, https://pubchem.ncbi.nlm.nih.gov/compound/44603531.</ref> stops the hepatitis C virus by inhibiting the NS3/4A protease, which is an enzyme responsible for the cleavage of the viral polyprotein. 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 <scene name='74/746120/P2-p4_macrocylic_ring/1'>P2 to P4 macrocyclic restriction</scene>, which interacts with the catalytic triad of the NS3/4A protease in its own distinct conformation. Due to this conformation, Grazoprevir can easily bind to the catalytic triad because it is already in a highly favorable arrangement, stopping the triads activity.<ref>DOI: 10.1021/acschembio.5b00647</ref>.

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Revision as of 20:41, 4 December 2016 view source Megan Harris. (talk \| contribs) 72 edits No edit summary ← Older edit		Revision as of 17:41, 5 December 2016 view source Ruby Danielle Lee (talk \| contribs) 22 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> (C<sub>38</sub>H<sub>50</sub>N<sub>6</sub>O<sub>9</sub>, molecular weight: 766.911 g/mol) <ref>National Center for Biotechnology Information. PubChem Compound Database; CID=44603531, https://pubchem.ncbi.nlm.nih.gov/compound/44603531.</ref> stops the hepatitis C virus by inhibiting the NS3/4A protease, which is an enzyme responsible for the cleavage of the viral polyprotein. 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. Due to this conformation, Grazoprevir can easily bind to the catalytic triad because it is already in a highly favorable arrangement, stopping the triads activity.<ref>DOI: 10.1021/acschembio.5b00647</ref>.		<scene name='74/745998/Grazoprevir/3'>Grazoprevir</scene> (C<sub>38</sub>H<sub>50</sub>N<sub>6</sub>O<sub>9</sub>, molecular weight: 766.911 g/mol) <ref>National Center for Biotechnology Information. PubChem Compound Database; CID=44603531, https://pubchem.ncbi.nlm.nih.gov/compound/44603531.</ref> stops the hepatitis C virus by inhibiting the NS3/4A protease, which is an enzyme responsible for the cleavage of the viral polyprotein. 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 <scene name='74/746120/P2-p4_macrocylic_ring/1'>P2 to P4 macrocyclic restriction</scene>, which interacts with the catalytic triad of the NS3/4A protease in its own distinct conformation. Due to this conformation, Grazoprevir can easily bind to the catalytic triad because it is already in a highly favorable arrangement, stopping the triads activity.<ref>DOI: 10.1021/acschembio.5b00647</ref>.