1waw

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{{STRUCTURE_1waw| PDB=1waw | SCENE= }}
{{STRUCTURE_1waw| PDB=1waw | SCENE= }}
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'''SPECIFICITY AND AFFINITY OF NATURAL PRODUCT CYCLOPENTAPEPTIDE INHIBITOR ARGADIN AGAINST HUMAN CHITINASE'''
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===SPECIFICITY AND AFFINITY OF NATURAL PRODUCT CYCLOPENTAPEPTIDE INHIBITOR ARGADIN AGAINST HUMAN CHITINASE===
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==Overview==
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Family 18 chitinases play key roles in organisms ranging from bacteria to man. There is a need for specific, potent inhibitors to probe the function of these chitinases in different organisms. Such molecules could also provide leads for the development of chemotherapeuticals with fungicidal, insecticidal, or anti-inflammatory potential. Recently, two natural product peptides, argifin and argadin, have been characterized, which structurally mimic chitinase-chitooligosaccharide interactions and inhibit a bacterial chitinase in the nM-mM range. Here, we show that these inhibitors also act on human and Aspergillus fumigatus chitinases. The structures of these enzymes in complex with argifin and argadin, together with mutagenesis, fluorescence, and enzymology, reveal that subtle changes in the binding site dramatically affect affinity and selectivity. The data show that it may be possible to develop specific chitinase inhibitors based on the argifin/argadin scaffolds.
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(as it appears on PubMed at http://www.pubmed.gov), where 15664516 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15664516}}
==About this Structure==
==About this Structure==
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[[Category: Human chitinase]]
[[Category: Human chitinase]]
[[Category: Hydrolase]]
[[Category: Hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 13:23:55 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 08:29:06 2008''

Revision as of 05:29, 29 July 2008

Image:1waw.png

Template:STRUCTURE 1waw

SPECIFICITY AND AFFINITY OF NATURAL PRODUCT CYCLOPENTAPEPTIDE INHIBITOR ARGADIN AGAINST HUMAN CHITINASE

Template:ABSTRACT PUBMED 15664516

About this Structure

1WAW is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases., Rao FV, Houston DR, Boot RG, Aerts JM, Hodkinson M, Adams DJ, Shiomi K, Omura S, van Aalten DM, Chem Biol. 2005 Jan;12(1):65-76. PMID:15664516

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