1t7k
From Proteopedia
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| - | [[Image:1t7k.gif|left|200px]] | + | [[Image:1t7k.gif|left|200px]] |
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| - | '''Crystal Structure of HIV Protease complexed with Arylsulfonamide azacyclic urea''' | + | {{Structure |
| + | |PDB= 1t7k |SIZE=350|CAPTION= <scene name='initialview01'>1t7k</scene>, resolution 2.10Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=BH0:3-({5-BENZYL-6-HYDROXY-2,4-BIS-(4-HYDROXY-BENZYL)-3-OXO-[1,2,4]-TRIAZEPANE-1-SULFONYL)-BENZONITRILE'>BH0</scene> | ||
| + | |ACTIVITY= [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] | ||
| + | |GENE= POL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=11676 Human immunodeficiency virus 1]) | ||
| + | }} | ||
| + | |||
| + | '''Crystal Structure of HIV Protease complexed with Arylsulfonamide azacyclic urea''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1T7K is a [ | + | 1T7K is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T7K OCA]. |
==Reference== | ==Reference== | ||
| - | Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors., Huang PP, Randolph JT, Klein LL, Vasavanonda S, Dekhtyar T, Stoll VS, Kempf DJ, Bioorg Med Chem Lett. 2004 Aug 2;14(15):4075-8. PMID:[http:// | + | Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors., Huang PP, Randolph JT, Klein LL, Vasavanonda S, Dekhtyar T, Stoll VS, Kempf DJ, Bioorg Med Chem Lett. 2004 Aug 2;14(15):4075-8. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15225729 15225729] |
[[Category: HIV-1 retropepsin]] | [[Category: HIV-1 retropepsin]] | ||
[[Category: Human immunodeficiency virus 1]] | [[Category: Human immunodeficiency virus 1]] | ||
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[[Category: hiv protease]] | [[Category: hiv protease]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:14:51 2008'' |
Revision as of 12:14, 20 March 2008
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| , resolution 2.10Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | POL (Human immunodeficiency virus 1) | ||||||
| Activity: | HIV-1 retropepsin, with EC number 3.4.23.16 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal Structure of HIV Protease complexed with Arylsulfonamide azacyclic urea
Overview
A series of novel azacyclic urea HIV protease inhibitors bearing a benzenesulfonamide group at P1' were synthesized utilizing a parallel synthesis method. Structural studies of early analogs bound in the enzyme active site were used to design more potent inhibitors. The effects of substituting the P1' benzenesulfonyl group on antiviral activity and protein binding are described.
About this Structure
1T7K is a Single protein structure of sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.
Reference
Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors., Huang PP, Randolph JT, Klein LL, Vasavanonda S, Dekhtyar T, Stoll VS, Kempf DJ, Bioorg Med Chem Lett. 2004 Aug 2;14(15):4075-8. PMID:15225729
Page seeded by OCA on Thu Mar 20 14:14:51 2008
