2p59: Difference between revisions

Line 1:

[[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==

is a [http://en.wikipedia.org/wiki/~~Protein_complex Protein complex~~] structure of ~~sequences~~ from [http://en.wikipedia.org/wiki/ ]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id= OCA].

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: ~~Protein complex~~]]

==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 15:34:39 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 6 17:23:10 2008''

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@@ Line 1: / Line 1: @@
 [[Image:2p59.jpg|left|200px]]<br /><applet load="2p59" size="350" color="white" frame="true" align="right" spinBox="true"
-caption="2p59" />
+caption="2p59, resolution 2.900&Aring;" />
-''''''<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==
- is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/ ]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id= OCA].
+P59 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: Protein complex]]
+==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 15:34:39 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb  6 17:23:10 2008''