2p59
From Proteopedia
(New page: 200px<br /><applet load="2p59" size="350" color="white" frame="true" align="right" spinBox="true" caption="2p59" /> ''''''<br /> ==About this Structure== is a [h...) |
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[[Image:2p59.jpg|left|200px]]<br /><applet load="2p59" size="350" color="white" frame="true" align="right" spinBox="true" | [[Image:2p59.jpg|left|200px]]<br /><applet load="2p59" size="350" color="white" frame="true" align="right" spinBox="true" | ||
| - | caption="2p59" /> | + | caption="2p59, resolution 2.900Å" /> |
| - | ''''''<br /> | + | '''Crystal Structure of Hepatitis C Virus NS3.4A protease'''<br /> |
| + | |||
| + | ==Overview== | ||
| + | Reversible tetrapeptide-based compounds have been shown to effectively, inhibit the hepatitis C virus NS3.4A protease. Inhibition of viral, replicon RNA production in Huh-7 cells has also been demonstrated. We show, herein that the inclusion of hydrogen bond donors on the P4 capping group, of tetrapeptide-based inhibitors result in increased binding potency to, the NS3.4A protease. The capping groups also impart significant effects on, the pharmacokinetic profile of these inhibitors. | ||
==About this Structure== | ==About this Structure== | ||
| - | + | 2P59 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Gb_virus_c Gb virus c] with <scene name='pdbligand=GG4:'>GG4</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:Gg4+Binding+Site+For+Residue+B+1208'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2P59 OCA]. | |
| - | [[Category: | + | |
| + | ==Reference== | ||
| + | Inhibitors of hepatitis C virus NS3.4A protease. Effect of P4 capping groups on inhibitory potency and pharmacokinetics., Perni RB, Chandorkar G, Cottrell KM, Gates CA, Lin C, Lin K, Luong YP, Maxwell JP, Murcko MA, Pitlik J, Rao G, Schairer WC, Van Drie J, Wei Y, Bioorg Med Chem Lett. 2007 Jun 15;17(12):3406-11. Epub 2007 Apr 3. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17482818 17482818] | ||
| + | [[Category: Gb virus c]] | ||
| + | [[Category: Single protein]] | ||
| + | [[Category: Perni, R.B.]] | ||
| + | [[Category: Wei, Y.]] | ||
| + | [[Category: GG4]] | ||
| + | [[Category: hcv protease]] | ||
| + | [[Category: viral protein]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 6 | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 6 17:23:10 2008'' |
Revision as of 15:23, 6 February 2008
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Crystal Structure of Hepatitis C Virus NS3.4A protease
Overview
Reversible tetrapeptide-based compounds have been shown to effectively, inhibit the hepatitis C virus NS3.4A protease. Inhibition of viral, replicon RNA production in Huh-7 cells has also been demonstrated. We show, herein that the inclusion of hydrogen bond donors on the P4 capping group, of tetrapeptide-based inhibitors result in increased binding potency to, the NS3.4A protease. The capping groups also impart significant effects on, the pharmacokinetic profile of these inhibitors.
About this Structure
2P59 is a Single protein structure of sequence from Gb virus c with as ligand. Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
Inhibitors of hepatitis C virus NS3.4A protease. Effect of P4 capping groups on inhibitory potency and pharmacokinetics., Perni RB, Chandorkar G, Cottrell KM, Gates CA, Lin C, Lin K, Luong YP, Maxwell JP, Murcko MA, Pitlik J, Rao G, Schairer WC, Van Drie J, Wei Y, Bioorg Med Chem Lett. 2007 Jun 15;17(12):3406-11. Epub 2007 Apr 3. PMID:17482818
Page seeded by OCA on Wed Feb 6 17:23:10 2008
Categories: Gb virus c | Single protein | Perni, R.B. | Wei, Y. | GG4 | Hcv protease | Viral protein
