1rtl
From Proteopedia
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'''CRYSTAL STRUCTURE OF HCV NS3 PROTEASE DOMAIN: NS4A PEPTIDE COMPLEX WITH COVALENTLY BOUND PYRROLIDINE-5,5-TRANSLACTAM INHIBITOR''' | '''CRYSTAL STRUCTURE OF HCV NS3 PROTEASE DOMAIN: NS4A PEPTIDE COMPLEX WITH COVALENTLY BOUND PYRROLIDINE-5,5-TRANSLACTAM INHIBITOR''' | ||
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[[Category: Skarzynski, T.]] | [[Category: Skarzynski, T.]] | ||
[[Category: Somers, D O.N.]] | [[Category: Somers, D O.N.]] | ||
- | [[Category: | + | [[Category: Cofactor peptide]] |
- | [[Category: | + | [[Category: Helicase]] |
- | [[Category: | + | [[Category: Inhibitor]] |
- | [[Category: | + | [[Category: Nonstructural protein]] |
- | [[Category: | + | [[Category: Serine protease]] |
- | [[Category: | + | [[Category: Translactam]] |
- | [[Category: | + | [[Category: Viral protein]] |
- | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:53:27 2008'' | |
- | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + |
Revision as of 04:53, 3 May 2008
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. 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 Sat May 3 07:53:27 2008