2a4f

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[[Image:2a4f.gif|left|200px]]
[[Image:2a4f.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2a4f |SIZE=350|CAPTION= <scene name='initialview01'>2a4f</scene>, resolution 1.90&Aring;
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The line below this paragraph, containing "STRUCTURE_2a4f", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=AAU:(5R,6R)-5-BENZYL-6-HYDROXY-2,4-BIS(4-HYDROXY-3-METHOXYBENZYL)-1-[3-(4-HYDROXYPHENYL)PROPANOYL]-1,2,4-TRIAZEPAN-3-ONE'>AAU</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/HIV-1_retropepsin HIV-1 retropepsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.16 3.4.23.16] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= POL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=11676 Human immunodeficiency virus 1])
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-->
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|DOMAIN=
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{{STRUCTURE_2a4f| PDB=2a4f | SCENE= }}
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|RELATEDENTRY=[[1yt9|1YT9]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2a4f FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2a4f OCA], [http://www.ebi.ac.uk/pdbsum/2a4f PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2a4f RCSB]</span>
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}}
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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.'''
'''Synthesis and Activity of N-Axyl Azacyclic Urea HIV-1 Protease Inhibitors with High Potency Against Multiple Drug Resistant Viral Strains.'''
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[[Category: Vasavanonda, S.]]
[[Category: Vasavanonda, S.]]
[[Category: Zhao, C.]]
[[Category: Zhao, C.]]
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[[Category: aza-cyclic urea]]
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[[Category: Aza-cyclic urea]]
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[[Category: hiv protease]]
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[[Category: Hiv protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 18:35:18 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:47:45 2008''
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Revision as of 15:35, 3 May 2008

Image:2a4f.gif

Template:STRUCTURE 2a4f

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. 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 Sat May 3 18:35:18 2008

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