1yt9
From Proteopedia
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==Overview== | ==Overview== | ||
| - | The need for a potent HIV protease inhibitor (PI) to combat emerging | + | The need for a potent HIV protease inhibitor (PI) to combat emerging PI-resistant viruses is anticipated. Analogs formulated from the combination of structural fragments of Ritonavir, Lopinavir, and Amprenavir were synthesized. Analogs containing the oxime pharmacophore were found to have improved activities against both wild type and resistant (A17) viruses. The synthesis and structure-activity relationships (SAR) based upon the in vitro IC50 of this series of compounds are reported. |
==About this Structure== | ==About this Structure== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Dekhtyar, T.]] | [[Category: Dekhtyar, T.]] | ||
| - | [[Category: Flentge, C | + | [[Category: Flentge, C A.]] |
| - | [[Category: Kempf, D | + | [[Category: Kempf, D J.]] |
| - | [[Category: Klein, L | + | [[Category: Klein, L L.]] |
| - | [[Category: Randolph, J | + | [[Category: Randolph, J T.]] |
| - | [[Category: Stoll, V | + | [[Category: Stoll, V S.]] |
[[Category: Sun, M.]] | [[Category: Sun, M.]] | ||
| - | [[Category: Yeung, C | + | [[Category: Yeung, C M.]] |
[[Category: Zhao, C.]] | [[Category: Zhao, C.]] | ||
[[Category: OIS]] | [[Category: OIS]] | ||
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[[Category: oximinoarylsulfonamides]] | [[Category: oximinoarylsulfonamides]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:08:54 2008'' |
Revision as of 14:09, 21 February 2008
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HIV Protease with oximinoarylsulfonamide bound
Overview
The need for a potent HIV protease inhibitor (PI) to combat emerging PI-resistant viruses is anticipated. Analogs formulated from the combination of structural fragments of Ritonavir, Lopinavir, and Amprenavir were synthesized. Analogs containing the oxime pharmacophore were found to have improved activities against both wild type and resistant (A17) viruses. The synthesis and structure-activity relationships (SAR) based upon the in vitro IC50 of this series of compounds are reported.
About this Structure
1YT9 is a Single protein structure of sequence from Human immunodeficiency virus 1 with as ligand. Full crystallographic information is available from OCA.
Reference
Oximinoarylsulfonamides as potent HIV protease inhibitors., Yeung CM, Klein LL, Flentge CA, Randolph JT, Zhao C, Sun M, Dekhtyar T, Stoll VS, Kempf DJ, Bioorg Med Chem Lett. 2005 May 2;15(9):2275-8. PMID:15837308
Page seeded by OCA on Thu Feb 21 16:08:54 2008
