5jyy
From Proteopedia
(Difference between revisions)
(New page: '''Unreleased structure''' The entry 5jyy is ON HOLD Authors: Fu, L., Wu, Y., Bi, Y., Zhang, S., Lv, X., Qi, J., Li, Y., Lu, X., Yan, J., Gao, G.F., Li, X. Description: Structure-based...) |
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| - | '''Unreleased structure''' | ||
| - | + | ==Structure-based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-resistant Influenza Viruses== | |
| + | <StructureSection load='5jyy' size='340' side='right'caption='[[5jyy]], [[Resolution|resolution]] 2.10Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5jyy]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Influenza_A_virus Influenza A virus]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=5e6l 5e6l]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5JYY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5JYY FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.1Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6PY:5-(ACETYLAMINO)-2,6-ANHYDRO-4-CARBAMIMIDAMIDO-3,4,5-TRIDEOXY-7-O-[(2-METHOXYETHYL)CARBAMOYL]-D-GLYCERO-D-GALACTO-NON-2-ENONIC+ACID'>6PY</scene>, <scene name='pdbligand=BMA:BETA-D-MANNOSE'>BMA</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=MAN:ALPHA-D-MANNOSE'>MAN</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5jyy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5jyy OCA], [https://pdbe.org/5jyy PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5jyy RCSB], [https://www.ebi.ac.uk/pdbsum/5jyy PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5jyy ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/R4NFR6_9INFA R4NFR6_9INFA] Catalyzes the removal of terminal sialic acid residues from viral and cellular glycoconjugates.[RuleBase:RU361252] | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Zanamivir and oseltamivir are principal influenza antiviral drugs that target viral neuraminidase (NA), but resistant viruses containing mutant NAs with diminished drug affinity are increasingly emerging. Using the structural knowledge of both drug-binding sites and their spatial arrangement on the homotetrameric NA, we have developed a tetravalent zanamivir (TZ) molecule that exhibited marked increases in NA binding affinity, inhibition of NA enzyme activity, and in vitro plus in vivo antiviral efficacy over zanamivir. TZ functioned against both human seasonal H3N2 and avian H7N9 viruses, including drug-resistant mutants. Crystal structure of a resistant N9 NA in complex with TZ explained the function, which showed that four zanamivir residues simultaneously bound to all four monomers of NA. The design method of TZ described in this study may be useful to develop drugs or ligands that target proteins with multiple binding sites. The potent anti-influenza activity of TZ makes it attractive for further development. | ||
| - | + | Structure-Based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-Resistant Influenza Viruses.,Fu L, Bi Y, Wu Y, Zhang S, Qi J, Li Y, Lu X, Zhang Z, Lv X, Yan J, Gao GF, Li X J Med Chem. 2016 Jul 6. PMID:27341624<ref>PMID:27341624</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: | + | <div class="pdbe-citations 5jyy" style="background-color:#fffaf0;"></div> |
| - | [[Category: | + | |
| - | [[Category: | + | ==See Also== |
| - | [[Category: | + | *[[Neuraminidase 3D structures|Neuraminidase 3D structures]] |
| - | [[Category: | + | == References == |
| - | [[Category: | + | <references/> |
| - | [[Category: Lu | + | __TOC__ |
| - | [[Category: | + | </StructureSection> |
| - | [[Category: | + | [[Category: Influenza A virus]] |
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: | + | [[Category: Bi Y]] |
| + | [[Category: Fu L]] | ||
| + | [[Category: Gao GF]] | ||
| + | [[Category: Li X]] | ||
| + | [[Category: Li Y]] | ||
| + | [[Category: Lu X]] | ||
| + | [[Category: Lv X]] | ||
| + | [[Category: Qi J]] | ||
| + | [[Category: Wu Y]] | ||
| + | [[Category: Yan J]] | ||
| + | [[Category: Zhang S]] | ||
Current revision
Structure-based Tetravalent Zanamivir with Potent Inhibitory Activity against Drug-resistant Influenza Viruses
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Categories: Influenza A virus | Large Structures | Bi Y | Fu L | Gao GF | Li X | Li Y | Lu X | Lv X | Qi J | Wu Y | Yan J | Zhang S
