1o6i

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[[Image:1o6i.jpg|left|200px]]
[[Image:1o6i.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1o6i |SIZE=350|CAPTION= <scene name='initialview01'>1o6i</scene>, resolution 1.70&Aring;
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The line below this paragraph, containing "STRUCTURE_1o6i", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=ARB:ARG+Binding+Site+For+Chain+A'>ARB</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=DPR:D-PROLINE'>DPR</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Hydrolase Hydrolase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.14. 3.2.1.14.] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1o6i| PDB=1o6i | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1o6i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1o6i OCA], [http://www.ebi.ac.uk/pdbsum/1o6i PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1o6i RCSB]</span>
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}}
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'''CHITINASE B FROM SERRATIA MARCESCENS COMPLEXED WITH THE CATALYTIC INTERMEDIATE MIMIC CYCLIC DIPEPTIDE CI4.'''
'''CHITINASE B FROM SERRATIA MARCESCENS COMPLEXED WITH THE CATALYTIC INTERMEDIATE MIMIC CYCLIC DIPEPTIDE CI4.'''
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[[Category: Houston, D R.]]
[[Category: Houston, D R.]]
[[Category: Synstad, B.]]
[[Category: Synstad, B.]]
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[[Category: catalytic intermediate mimic]]
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[[Category: Catalytic intermediate mimic]]
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[[Category: chitinase]]
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[[Category: Chitinase]]
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[[Category: cyclic dipeptide,hydrolase]]
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[[Category: Cyclic dipeptide,hydrolase]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 03:26:36 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:40:33 2008''
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Revision as of 00:26, 3 May 2008

Image:1o6i.jpg

Template:STRUCTURE 1o6i

CHITINASE B FROM SERRATIA MARCESCENS COMPLEXED WITH THE CATALYTIC INTERMEDIATE MIMIC CYCLIC DIPEPTIDE CI4.


Overview

Family 18 chitinases are attractive targets for the development of new inhibitors with chemotherapeutic potential against fungi, insects and protozoan/nematodal parasites. Although several inhibitors have been identified, these are based on complex chemistry, which hampers iterative structure-based optimization. Here we report the details of chitinase inhibition by the natural product peptide CI-4 [ cyclo -(L-Arg-D-Pro)], which possesses activity against the human pathogenic fungus Candida albicans, and describe a 1.7 A (0.17 nm) crystal structure of CI-4 in complex with the enzyme. The structure reveals that the cyclic dipeptide inhibits chitinases by structurally mimicking a reaction intermediate, and could, on the basis of its accessible chemistry, be a candidate for further optimization.

About this Structure

1O6I is a Single protein structure of sequence from Serratia marcescens. Full crystallographic information is available from OCA.

Reference

The cyclic dipeptide CI-4 [cyclo-(l-Arg-d-Pro)] inhibits family 18 chitinases by structural mimicry of a reaction intermediate., Houston DR, Eggleston I, Synstad B, Eijsink VG, van Aalten DM, Biochem J. 2002 Nov 15;368(Pt 1):23-7. PMID:12323074 Page seeded by OCA on Sat May 3 03:26:36 2008

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