1dy9: Difference between revisions
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New page: left|200px<br /><applet load="1dy9" size="450" color="white" frame="true" align="right" spinBox="true" caption="1dy9, resolution 2.1Å" /> '''INHIBITION OF THE HEP... |
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[[Image:1dy9.gif|left|200px]]<br /><applet load="1dy9" size=" | [[Image:1dy9.gif|left|200px]]<br /><applet load="1dy9" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="1dy9, resolution 2.1Å" /> | caption="1dy9, resolution 2.1Å" /> | ||
'''INHIBITION OF THE HEPATITIS C VIRUS NS3/4A PROTEASE. THE CRYSTAL STRUCTURES OF TWO PROTEASE-INHIBITOR COMPLEXES (INHIBITOR I)'''<br /> | '''INHIBITION OF THE HEPATITIS C VIRUS NS3/4A PROTEASE. THE CRYSTAL STRUCTURES OF TWO PROTEASE-INHIBITOR COMPLEXES (INHIBITOR I)'''<br /> | ||
==Overview== | ==Overview== | ||
The hepatitis C virus NS3 protein contains a serine protease domain with a | The hepatitis C virus NS3 protein contains a serine protease domain with a chymotrypsin-like fold, which is a target for development of therapeutics. We report the crystal structures of this domain complexed with NS4A cofactor and with two potent, reversible covalent inhibitors spanning the P1-P4 residues. Both inhibitors bind in an extended backbone conformation, forming an anti-parallel beta-sheet with one enzyme beta-strand. The P1 residue contributes most to the binding energy, whereas P2-P4 side chains are partially solvent exposed. The structures do not show notable rearrangements of the active site upon inhibitor binding. These results are significant for the development of antivirals. | ||
==About this Structure== | ==About this Structure== | ||
1DY9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Viruses Viruses] with ZN as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | 1DY9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Viruses Viruses] with <scene name='pdbligand=ZN:'>ZN</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1DY9 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Viruses]] | [[Category: Viruses]] | ||
[[Category: Colarusso, S.]] | [[Category: Colarusso, S.]] | ||
[[Category: Francesco, R | [[Category: Francesco, R De.]] | ||
[[Category: Marco, S | [[Category: Marco, S Di.]] | ||
[[Category: Matassa, V | [[Category: Matassa, V G.]] | ||
[[Category: Narjes, F.]] | [[Category: Narjes, F.]] | ||
[[Category: Rizzi, M.]] | [[Category: Rizzi, M.]] | ||
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[[Category: serine protease]] | [[Category: serine protease]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:21:46 2008'' | ||
