1wb0

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[[Image:1wb0.gif|left|200px]]<br /><applet load="1wb0" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1wb0.gif|left|200px]]
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caption="1wb0, resolution 1.65&Aring;" />
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'''SPECIFICITY AND AFFINITY OF NATURAL PRODUCT CYCLOPENTAPEPTIDE INHIBITOR ARGIFIN AGAINST HUMAN CHITINASE'''<br />
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{{Structure
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|PDB= 1wb0 |SIZE=350|CAPTION= <scene name='initialview01'>1wb0</scene>, resolution 1.65&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=RAG:ARGIFIN'>RAG</scene>, <scene name='pdbligand=IPA:ISOPROPYL+ALCOHOL'>IPA</scene> and <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>
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|ACTIVITY= [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]
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|GENE=
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}}
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'''SPECIFICITY AND AFFINITY OF NATURAL PRODUCT CYCLOPENTAPEPTIDE INHIBITOR ARGIFIN AGAINST HUMAN CHITINASE'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1WB0 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 <scene name='pdbligand=SO4:'>SO4</scene>, <scene name='pdbligand=RAG:'>RAG</scene>, <scene name='pdbligand=IPA:'>IPA</scene> and <scene name='pdbligand=GOL:'>GOL</scene> 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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WB0 OCA].
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1WB0 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WB0 OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15664516 15664516]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/15664516 15664516]
[[Category: Chitinase]]
[[Category: Chitinase]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: chitin degradation]]
[[Category: chitin degradation]]
[[Category: chitin-binding]]
[[Category: chitin-binding]]
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[[Category: chitinase inhibitors]]
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[[Category: chitinase inhibitor]]
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[[Category: cyclopentapeptide inhibitors]]
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[[Category: cyclopentapeptide inhibitor]]
[[Category: glycosidase]]
[[Category: glycosidase]]
[[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 Thu Feb 21 15:42:22 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:54:36 2008''

Revision as of 12:54, 20 March 2008

Image:1wb0.gif


PDB ID 1wb0

Drag the structure with the mouse to rotate
, resolution 1.65Å
Ligands: , , and
Activity: Chitinase, with EC number 3.2.1.14
Coordinates: save as pdb, mmCIF, xml



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


Overview

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 Structure

1WB0 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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