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1ing

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{{STRUCTURE_1ing| PDB=1ing | SCENE= }}
{{STRUCTURE_1ing| PDB=1ing | SCENE= }}
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'''INFLUENZA A SUBTYPE N2 NEURAMINIDASE COMPLEXED WITH AROMATIC BANA109 INHIBITOR'''
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===INFLUENZA A SUBTYPE N2 NEURAMINIDASE COMPLEXED WITH AROMATIC BANA109 INHIBITOR===
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==Overview==
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Influenza virus sialidase is a surface enzyme that is essential for infection of the virus. The catalytic site is highly conserved among all known influenza variants, suggesting that this protein is a suitable target for drug intervention. The most potent known inhibitors are analogs of 2-deoxy-2,3-didehydro-N-acetylneuraminic acid (Neu5Ac2en), particularly the 4-guanidino derivative (4-guanidino-Neu5Ac2en). We utilized the benzene ring of 4-(N-acetylamino)benzoic acids as a cyclic template to substitute for the dihydropyran ring of Neu5Ac2en. In this study several 3-(N-acylamino) derivatives were prepared as potential replacements for the glycerol side chain of Neu5Ac2en, and some were found to interact with the same binding subsite of sialidase. Of greater significance was the observation that the 3-guanidinobenzoic acid derivative (equivalent to the 4-guanidino grouping of 4-guanidino-Neu5Ac2en), the most potent benzoic acid inhibitor of influenza sialidase thus far identified (IC50 = 10 microM), occupied the glycerol-binding subsite on sialidase as opposed to the guanidino-binding subsite. This benzoic acid derivative thus provides a new compound that interacts in a novel manner with the catalytic site of influenza sialidase.
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(as it appears on PubMed at http://www.pubmed.gov), where 7650674 is the PubMed ID number.
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{{ABSTRACT_PUBMED_7650674}}
==About this Structure==
==About this Structure==
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[[Category: O-glycosyl]]
[[Category: O-glycosyl]]
[[Category: Sialidase]]
[[Category: Sialidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 20:11:18 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 13:36:18 2008''

Revision as of 10:36, 1 July 2008

Image:1ing.png

Template:STRUCTURE 1ing

INFLUENZA A SUBTYPE N2 NEURAMINIDASE COMPLEXED WITH AROMATIC BANA109 INHIBITOR

Template:ABSTRACT PUBMED 7650674

About this Structure

1ING is a Single protein structure of sequence from Influenza a virus subtype n2. Full crystallographic information is available from OCA.

Reference

Structure-based inhibitors of influenza virus sialidase. A benzoic acid lead with novel interaction., Singh S, Jedrzejas MJ, Air GM, Luo M, Laver WG, Brouillette WJ, J Med Chem. 1995 Aug 18;38(17):3217-25. PMID:7650674

Page seeded by OCA on Tue Jul 1 13:36:18 2008

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