1waw: Difference between revisions
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[[Image:1waw.gif|left|200px]]<br /> | [[Image:1waw.gif|left|200px]]<br /><applet load="1waw" size="450" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="1waw" size="450" color="white" frame="true" align="right" spinBox="true" | |||
caption="1waw, resolution 1.75Å" /> | caption="1waw, resolution 1.75Å" /> | ||
'''SPECIFICITY AND AFFINITY OF NATURAL PRODUCT CYCLOPENTAPEPTIDE INHIBITOR ARGADIN AGAINST HUMAN CHITINASE'''<br /> | '''SPECIFICITY AND AFFINITY OF NATURAL PRODUCT CYCLOPENTAPEPTIDE INHIBITOR ARGADIN AGAINST HUMAN CHITINASE'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
1WAW is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4, RIG, GOL and IPA as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Chitinase Chitinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.14 3.2.1.14] | 1WAW is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4, RIG, GOL and IPA as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Chitinase Chitinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.14 3.2.1.14] Known structural/functional Site: <scene name='pdbsite=AC1:So4 Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1WAW OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: hydrolase]] | [[Category: hydrolase]] | ||
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Revision as of 19:26, 18 December 2007
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SPECIFICITY AND AFFINITY OF NATURAL PRODUCT CYCLOPENTAPEPTIDE INHIBITOR ARGADIN AGAINST HUMAN CHITINASE
OverviewOverview
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.
About this StructureAbout this Structure
1WAW is a Single protein structure of sequence from Homo sapiens with SO4, RIG, GOL and IPA as ligands. Active as Chitinase, with EC number 3.2.1.14 Known structural/functional Site: . Full crystallographic information is available from OCA.
ReferenceReference
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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