1o6i

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{{Seed}}
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{{STRUCTURE_1o6i| PDB=1o6i | SCENE= }}
{{STRUCTURE_1o6i| PDB=1o6i | SCENE= }}
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'''CHITINASE B FROM SERRATIA MARCESCENS COMPLEXED WITH THE CATALYTIC INTERMEDIATE MIMIC CYCLIC DIPEPTIDE CI4.'''
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===CHITINASE B FROM SERRATIA MARCESCENS COMPLEXED WITH THE CATALYTIC INTERMEDIATE MIMIC CYCLIC DIPEPTIDE CI4.===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 12323074 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12323074}}
==About this Structure==
==About this Structure==
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[[Category: Cyclic dipeptide,hydrolase]]
[[Category: Cyclic dipeptide,hydrolase]]
[[Category: Inhibitor]]
[[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 Tue Jul 29 01:09:49 2008''

Revision as of 22:10, 28 July 2008

Image:1o6i.png

Template:STRUCTURE 1o6i

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

Template:ABSTRACT PUBMED 12323074

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

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