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From Proteopedia
(New page: 200px<br /><applet load="1rtl" size="450" color="white" frame="true" align="right" spinBox="true" caption="1rtl, resolution 2.75Å" /> '''CRYSTAL STRUCTURE OF...) |
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| - | [[Image:1rtl.gif|left|200px]]<br /><applet load="1rtl" size=" | + | [[Image:1rtl.gif|left|200px]]<br /><applet load="1rtl" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1rtl, resolution 2.75Å" /> | caption="1rtl, resolution 2.75Å" /> | ||
'''CRYSTAL STRUCTURE OF HCV NS3 PROTEASE DOMAIN: NS4A PEPTIDE COMPLEX WITH COVALENTLY BOUND PYRROLIDINE-5,5-TRANSLACTAM INHIBITOR'''<br /> | '''CRYSTAL STRUCTURE OF HCV NS3 PROTEASE DOMAIN: NS4A PEPTIDE COMPLEX WITH COVALENTLY BOUND PYRROLIDINE-5,5-TRANSLACTAM INHIBITOR'''<br /> | ||
==Overview== | ==Overview== | ||
| - | [reaction: see text] In this, the first of two Letters, we describe how a | + | [reaction: see text] In this, the first of two Letters, we describe how a P3/P4 urea linking unit was used to greatly enhance the biochemical and replicon potency of inhibitors based upon the pyrrolidine-5,5-trans-lactam template. Compound 7b demonstrated a 100 nM IC(50) in the replicon cell-based surrogate HCV assay. |
==About this Structure== | ==About this Structure== | ||
| - | 1RTL is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Hepatitis_c_virus Hepatitis c virus] with ZN and CPX as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1RTL is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Hepatitis_c_virus Hepatitis c virus] with <scene name='pdbligand=ZN:'>ZN</scene> and <scene name='pdbligand=CPX:'>CPX</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1RTL OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Skarzynski, T.]] | [[Category: Skarzynski, T.]] | ||
| - | [[Category: Somers, D | + | [[Category: Somers, D O.N.]] |
[[Category: CPX]] | [[Category: CPX]] | ||
[[Category: ZN]] | [[Category: ZN]] | ||
| Line 25: | Line 25: | ||
[[Category: viral protein]] | [[Category: viral protein]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:54:22 2008'' |
Revision as of 12:54, 21 February 2008
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CRYSTAL STRUCTURE OF HCV NS3 PROTEASE DOMAIN: NS4A PEPTIDE COMPLEX WITH COVALENTLY BOUND PYRROLIDINE-5,5-TRANSLACTAM INHIBITOR
Overview
[reaction: see text] In this, the first of two Letters, we describe how a P3/P4 urea linking unit was used to greatly enhance the biochemical and replicon potency of inhibitors based upon the pyrrolidine-5,5-trans-lactam template. Compound 7b demonstrated a 100 nM IC(50) in the replicon cell-based surrogate HCV assay.
About this Structure
1RTL is a Protein complex structure of sequences from Hepatitis c virus with and as ligands. Full crystallographic information is available from OCA.
Reference
Pyrrolidine-5,5-trans-lactams. 4. Incorporation of a P3/P4 urea leads to potent intracellular inhibitors of hepatitis C virus NS3/4A protease., Slater MJ, Amphlett EM, Andrews DM, Bamborough P, Carey SJ, Johnson MR, Jones PS, Mills G, Parry NR, Somers DO, Stewart AJ, Skarzynski T, Org Lett. 2003 Nov 27;5(24):4627-30. PMID:14627400
Page seeded by OCA on Thu Feb 21 14:54:22 2008
