2ht7
From Proteopedia
(New page: 200px<br /><applet load="2ht7" size="450" color="white" frame="true" align="right" spinBox="true" caption="2ht7, resolution 2.6Å" /> '''N8 neuraminidase in o...) |
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| - | [[Image:2ht7.gif|left|200px]]<br /><applet load="2ht7" size=" | + | [[Image:2ht7.gif|left|200px]]<br /><applet load="2ht7" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2ht7, resolution 2.6Å" /> | caption="2ht7, resolution 2.6Å" /> | ||
'''N8 neuraminidase in open complex with oseltamivir'''<br /> | '''N8 neuraminidase in open complex with oseltamivir'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The worldwide spread of H5N1 avian influenza has raised concerns that this | + | The worldwide spread of H5N1 avian influenza has raised concerns that this virus might acquire the ability to pass readily among humans and cause a pandemic. Two anti-influenza drugs currently being used to treat infected patients are oseltamivir (Tamiflu) and zanamivir (Relenza), both of which target the neuraminidase enzyme of the virus. Reports of the emergence of drug resistance make the development of new anti-influenza molecules a priority. Neuraminidases from influenza type A viruses form two genetically distinct groups: group-1 contains the N1 neuraminidase of the H5N1 avian virus and group-2 contains the N2 and N9 enzymes used for the structure-based design of current drugs. Here we show by X-ray crystallography that these two groups are structurally distinct. Group-1 neuraminidases contain a cavity adjacent to their active sites that closes on ligand binding. Our analysis suggests that it may be possible to exploit the size and location of the group-1 cavity to develop new anti-influenza drugs. |
==About this Structure== | ==About this Structure== | ||
| - | 2HT7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Influenza_a_virus Influenza a virus] with G39 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Exo-alpha-sialidase Exo-alpha-sialidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.18 3.2.1.18] Full crystallographic information is available from [http:// | + | 2HT7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Influenza_a_virus Influenza a virus] with <scene name='pdbligand=G39:'>G39</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Exo-alpha-sialidase Exo-alpha-sialidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.18 3.2.1.18] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HT7 OCA]. |
==Reference== | ==Reference== | ||
| Line 14: | Line 14: | ||
[[Category: Influenza a virus]] | [[Category: Influenza a virus]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Blackburn, G | + | [[Category: Blackburn, G M.]] |
| - | [[Category: Collins, P | + | [[Category: Collins, P J.]] |
| - | [[Category: Gamblin, S | + | [[Category: Gamblin, S J.]] |
| - | [[Category: Haire, L | + | [[Category: Haire, L F.]] |
| - | [[Category: Hay, A | + | [[Category: Hay, A J.]] |
| - | [[Category: Lin, Y | + | [[Category: Lin, Y P.]] |
| - | [[Category: Russell, R | + | [[Category: Russell, R J.]] |
| - | [[Category: Skehel, J | + | [[Category: Skehel, J J.]] |
| - | [[Category: Stevens, D | + | [[Category: Stevens, D J.]] |
[[Category: G39]] | [[Category: G39]] | ||
[[Category: n8]] | [[Category: n8]] | ||
| Line 28: | Line 28: | ||
[[Category: oseltamivir]] | [[Category: oseltamivir]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:45:27 2008'' |
Revision as of 15:45, 21 February 2008
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N8 neuraminidase in open complex with oseltamivir
Overview
The worldwide spread of H5N1 avian influenza has raised concerns that this virus might acquire the ability to pass readily among humans and cause a pandemic. Two anti-influenza drugs currently being used to treat infected patients are oseltamivir (Tamiflu) and zanamivir (Relenza), both of which target the neuraminidase enzyme of the virus. Reports of the emergence of drug resistance make the development of new anti-influenza molecules a priority. Neuraminidases from influenza type A viruses form two genetically distinct groups: group-1 contains the N1 neuraminidase of the H5N1 avian virus and group-2 contains the N2 and N9 enzymes used for the structure-based design of current drugs. Here we show by X-ray crystallography that these two groups are structurally distinct. Group-1 neuraminidases contain a cavity adjacent to their active sites that closes on ligand binding. Our analysis suggests that it may be possible to exploit the size and location of the group-1 cavity to develop new anti-influenza drugs.
About this Structure
2HT7 is a Single protein structure of sequence from Influenza a virus with as ligand. Active as Exo-alpha-sialidase, with EC number 3.2.1.18 Full crystallographic information is available from OCA.
Reference
The structure of H5N1 avian influenza neuraminidase suggests new opportunities for drug design., Russell RJ, Haire LF, Stevens DJ, Collins PJ, Lin YP, Blackburn GM, Hay AJ, Gamblin SJ, Skehel JJ, Nature. 2006 Sep 7;443(7107):45-9. Epub 2006 Aug 16. PMID:16915235
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