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1rtl

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Revision as of 21:06, 24 November 2007 by OCA (Talk | contribs)
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1rtl, resolution 2.75Å

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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 ZN and CPX 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

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