2a4f
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(New page: 200px<br /> <applet load="2a4f" size="450" color="white" frame="true" align="right" spinBox="true" caption="2a4f, resolution 1.90Å" /> '''Synthesis and Activ...)
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Revision as of 12:34, 8 November 2007
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Synthesis and Activity of N-Axyl Azacyclic Urea HIV-1 Protease Inhibitors with High Potency Against Multiple Drug Resistant Viral Strains.
Overview
As part of our efforts to identify potent HIV-1 protease inhibitors that, are active against resistant viral strains, structural modification of the, azacyclic urea (I) was undertaken by incorporating acyl groups as P(1)', ligands. The extensive SAR study has yielded a series of N-acyl azacyclic, ureas (II), which are highly potent against both wild-type and multiple, PI-resistant viral strains.
About this Structure
2A4F is a Single protein structure of sequence from Human immunodeficiency virus 1 with AAU as ligand. Active as HIV-1 retropepsin, with EC number 3.4.23.16 Full crystallographic information is available from OCA.
Reference
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains., Zhao C, Sham HL, Sun M, Stoll VS, Stewart KD, Lin S, Mo H, Vasavanonda S, Saldivar A, Park C, McDonald EJ, Marsh KC, Klein LL, Kempf DJ, Norbeck DW, Bioorg Med Chem Lett. 2005 Dec 15;15(24):5499-503. Epub 2005 Oct 3. PMID:16203141
Page seeded by OCA on Thu Nov 8 14:40:28 2007
