1cvr

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{{STRUCTURE_1cvr| PDB=1cvr | SCENE= }}
{{STRUCTURE_1cvr| PDB=1cvr | SCENE= }}
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'''CRYSTAL STRUCTURE OF THE ARG SPECIFIC CYSTEINE PROTEINASE GINGIPAIN R (RGPB)'''
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===CRYSTAL STRUCTURE OF THE ARG SPECIFIC CYSTEINE PROTEINASE GINGIPAIN R (RGPB)===
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==Overview==
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Gingipains are cysteine proteinases acting as key virulence factors of the bacterium Porphyromonas gingivalis, the major pathogen in periodontal disease. The 1.5 and 2.0 A crystal structures of free and D-Phe-Phe-Arg-chloromethylketone-inhibited gingipain R reveal a 435-residue, single-polypeptide chain organized into a catalytic and an immunoglobulin-like domain. The catalytic domain is subdivided into two subdomains comprising four- and six-stranded beta-sheets sandwiched by alpha-helices. Each subdomain bears topological similarities to the p20-p10 heterodimer of caspase-1. The second subdomain harbours the Cys-His catalytic diad and a nearby Glu arranged around the S1 specificity pocket, which carries an Asp residue to enforce preference for Arg-P1 residues. This gingipain R structure is an excellent template for the rational design of drugs with a potential to cure and prevent periodontitis. Here we show the binding mode of an arginine-containing inhibitor in the active-site, thus identifying major interaction sites defining a suitable pharmacophor.
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(as it appears on PubMed at http://www.pubmed.gov), where 10523290 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10523290}}
==About this Structure==
==About this Structure==
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[[Category: Caspase]]
[[Category: Caspase]]
[[Category: Cysteine proteinase]]
[[Category: Cysteine proteinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 13:09:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 21:32:16 2008''

Revision as of 18:32, 30 June 2008

Template:STRUCTURE 1cvr

CRYSTAL STRUCTURE OF THE ARG SPECIFIC CYSTEINE PROTEINASE GINGIPAIN R (RGPB)

Template:ABSTRACT PUBMED 10523290

About this Structure

1CVR is a Single protein structure of sequence from Porphyromonas gingivalis. Full crystallographic information is available from OCA.

Reference

Crystal structure of gingipain R: an Arg-specific bacterial cysteine proteinase with a caspase-like fold., Eichinger A, Beisel HG, Jacob U, Huber R, Medrano FJ, Banbula A, Potempa J, Travis J, Bode W, EMBO J. 1999 Oct 15;18(20):5453-62. PMID:10523290

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