1t7k
From Proteopedia
(New page: 200px<br /> <applet load="1t7k" size="450" color="white" frame="true" align="right" spinBox="true" caption="1t7k, resolution 2.10Å" /> '''Crystal Structure o...) |
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| - | [[Image:1t7k.gif|left|200px]]<br /> | + | [[Image:1t7k.gif|left|200px]]<br /><applet load="1t7k" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1t7k" size=" | + | |
caption="1t7k, resolution 2.10Å" /> | caption="1t7k, resolution 2.10Å" /> | ||
'''Crystal Structure of HIV Protease complexed with Arylsulfonamide azacyclic urea'''<br /> | '''Crystal Structure of HIV Protease complexed with Arylsulfonamide azacyclic urea'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A series of novel azacyclic urea HIV protease inhibitors bearing a | + | 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== | ==About this Structure== | ||
| - | 1T7K 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 BH0 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:// | + | 1T7K 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=BH0:'>BH0</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=1T7K OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Dekhtyar, T.]] | [[Category: Dekhtyar, T.]] | ||
| - | [[Category: Huang, P | + | [[Category: Huang, P P.]] |
| - | [[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: Vasavanonda, S.]] | [[Category: Vasavanonda, S.]] | ||
[[Category: BH0]] | [[Category: BH0]] | ||
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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 15:10:45 2008'' |
Revision as of 13:10, 21 February 2008
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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 with as ligand. Active as HIV-1 retropepsin, with EC number 3.4.23.16 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
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