1yt9: Difference between revisions
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|ACTIVITY= | |ACTIVITY= | ||
|GENE= POL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=11676 Human immunodeficiency virus 1]) | |GENE= POL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=11676 Human immunodeficiency virus 1]) | ||
|DOMAIN= | |||
|RELATEDENTRY=[[1mui|1MUI]] | |||
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yt9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yt9 OCA], [http://www.ebi.ac.uk/pdbsum/1yt9 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1yt9 RCSB]</span> | |||
}} | }} | ||
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[[Category: Yeung, C M.]] | [[Category: Yeung, C M.]] | ||
[[Category: Zhao, C.]] | [[Category: Zhao, C.]] | ||
[[Category: hiv protease]] | [[Category: hiv protease]] | ||
[[Category: oximinoarylsulfonamide]] | [[Category: oximinoarylsulfonamide]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:21:18 2008'' | ||
Revision as of 22:21, 30 March 2008
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| 1yt9, resolution 3.00Å | |||||||||||||
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| Ligands: | OIS | ||||||||||||
| Gene: | POL (Human immunodeficiency virus 1) | ||||||||||||
| Related: | 1MUI
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
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. 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
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