1dva

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{{STRUCTURE_1dva| PDB=1dva | SCENE= }}
{{STRUCTURE_1dva| PDB=1dva | SCENE= }}
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'''CRYSTAL STRUCTURE OF THE COMPLEX BETWEEN THE PEPTIDE EXOSITE INHIBITOR E-76 AND COAGULATION FACTOR VIIA'''
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===CRYSTAL STRUCTURE OF THE COMPLEX BETWEEN THE PEPTIDE EXOSITE INHIBITOR E-76 AND COAGULATION FACTOR VIIA===
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==Overview==
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Potent anticoagulants have been derived by targeting the tissue factor-factor VIIa complex with naive peptide libraries displayed on M13 phage. The peptides specifically block the activation of factor X with a median inhibitory concentration of 1 nM and selectively inhibit tissue-factor-dependent clotting. The peptides do not bind to the active site of factor VIIa; rather, they work by binding to an exosite on the factor VIIa protease domain, and non-competitively inhibit activation of factor X and amidolytic activity. One such peptide (E-76) has a well defined structure in solution determined by NMR spectroscopy that is similar to the X-ray crystal structure when complexed with factor VIIa. These structural and functional studies indicate an allosteric 'switch' mechanism of inhibition involving an activation loop of factor VIIa and represent a new framework for developing inhibitors of serine proteases.
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(as it appears on PubMed at http://www.pubmed.gov), where 10761907 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10761907}}
==About this Structure==
==About this Structure==
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[[Category: Ultsch, M H.]]
[[Category: Ultsch, M H.]]
[[Category: Protein-peptide complex]]
[[Category: Protein-peptide complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 14:19:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 23:40:17 2008''

Revision as of 20:40, 30 June 2008

Image:1dva.png

Template:STRUCTURE 1dva

CRYSTAL STRUCTURE OF THE COMPLEX BETWEEN THE PEPTIDE EXOSITE INHIBITOR E-76 AND COAGULATION FACTOR VIIA

Template:ABSTRACT PUBMED 10761907

About this Structure

1DVA is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Peptide exosite inhibitors of factor VIIa as anticoagulants., Dennis MS, Eigenbrot C, Skelton NJ, Ultsch MH, Santell L, Dwyer MA, O'Connell MP, Lazarus RA, Nature. 2000 Mar 30;404(6777):465-70. PMID:10761907

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