2ax0: Difference between revisions

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New page: left|200px<br /><applet load="2ax0" size="450" color="white" frame="true" align="right" spinBox="true" caption="2ax0, resolution 2.00Å" /> '''Hepatitis C Virus NS...
 
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[[Image:2ax0.gif|left|200px]]<br /><applet load="2ax0" size="450" color="white" frame="true" align="right" spinBox="true"  
[[Image:2ax0.gif|left|200px]]<br /><applet load="2ax0" size="350" color="white" frame="true" align="right" spinBox="true"  
caption="2ax0, resolution 2.00&Aring;" />
caption="2ax0, resolution 2.00&Aring;" />
'''Hepatitis C Virus NS5b RNA Polymerase in complex with a covalent inhibitor (5x)'''<br />
'''Hepatitis C Virus NS5b RNA Polymerase in complex with a covalent inhibitor (5x)'''<br />


==Overview==
==Overview==
Novel non-nucleoside inhibitors of the HCV RNA polymerase (NS5b) with, sub-micromolar biochemical potency have been identified which are, selective for the inhibition of HCV NS5b over other polymerases. The, structures of the complexes formed between several of these inhibitors and, HCV NS5b were determined by X-ray crystallography, and the inhibitors were, found to bind in an allosteric binding site separate from the active site., Structure-activity relationships and structural studies have identified, the mechanism of action for compounds in this series, several of which, possess drug-like properties, as unique, reversible, covalent inhibitors, of HCV NS5b.
Novel non-nucleoside inhibitors of the HCV RNA polymerase (NS5b) with sub-micromolar biochemical potency have been identified which are selective for the inhibition of HCV NS5b over other polymerases. The structures of the complexes formed between several of these inhibitors and HCV NS5b were determined by X-ray crystallography, and the inhibitors were found to bind in an allosteric binding site separate from the active site. Structure-activity relationships and structural studies have identified the mechanism of action for compounds in this series, several of which possess drug-like properties, as unique, reversible, covalent inhibitors of HCV NS5b.


==About this Structure==
==About this Structure==
2AX0 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Hepatitis_c_virus Hepatitis c virus] with SO4 and 5X as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/RNA-directed_RNA_polymerase RNA-directed RNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.48 2.7.7.48] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2AX0 OCA].  
2AX0 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Hepatitis_c_virus Hepatitis c virus] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=5X:'>5X</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/RNA-directed_RNA_polymerase RNA-directed RNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.48 2.7.7.48] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2AX0 OCA].  


==Reference==
==Reference==
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Anzola, J.]]
[[Category: Anzola, J.]]
[[Category: Chen, J.M.]]
[[Category: Chen, J M.]]
[[Category: Jaen, J.C.]]
[[Category: Jaen, J C.]]
[[Category: Lee, G.]]
[[Category: Lee, G.]]
[[Category: Li, Y.]]
[[Category: Li, Y.]]
[[Category: Liu, J.]]
[[Category: Liu, J.]]
[[Category: Mayorga, V.]]
[[Category: Mayorga, V.]]
[[Category: Peterson, M.G.]]
[[Category: Peterson, M G.]]
[[Category: Piper, D.E.]]
[[Category: Piper, D E.]]
[[Category: Powers, J.P.]]
[[Category: Powers, J P.]]
[[Category: Tonn, G.R.]]
[[Category: Tonn, G R.]]
[[Category: Walker, N.P.]]
[[Category: Walker, N P.]]
[[Category: Wang, Z.]]
[[Category: Wang, Z.]]
[[Category: Ye, Q.]]
[[Category: Ye, Q.]]
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[[Category: thumb]]
[[Category: thumb]]


''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Wed Nov 21 08:25:43 2007''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:31:50 2008''