2a4f: Difference between revisions
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New page: left|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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[[Image:2a4f.gif|left|200px]]<br /> | [[Image:2a4f.gif|left|200px]]<br /><applet load="2a4f" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="2a4f, resolution 1.90Å" /> | caption="2a4f, resolution 1.90Å" /> | ||
'''Synthesis and Activity of N-Axyl Azacyclic Urea HIV-1 Protease Inhibitors with High Potency Against Multiple Drug Resistant Viral Strains.'''<br /> | '''Synthesis and Activity of N-Axyl Azacyclic Urea HIV-1 Protease Inhibitors with High Potency Against Multiple Drug Resistant Viral Strains.'''<br /> | ||
==Overview== | ==Overview== | ||
As part of our efforts to identify potent HIV-1 protease inhibitors that | 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== | ==About this Structure== | ||
2A4F is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with AAU as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http:// | 2A4F is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with <scene name='pdbligand=AAU:'>AAU</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2A4F OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Saldivar, A.]] | [[Category: Saldivar, A.]] | ||
[[Category: Sham, H.]] | [[Category: Sham, H.]] | ||
[[Category: Stewart, K | [[Category: Stewart, K D.]] | ||
[[Category: Stoll, V.]] | [[Category: Stoll, V.]] | ||
[[Category: Sun, M.]] | [[Category: Sun, M.]] | ||
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[[Category: hiv protease]] | [[Category: hiv protease]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:23:34 2008'' | ||
