1dva: Difference between revisions
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New page: left|200px<br /> <applet load="1dva" size="450" color="white" frame="true" align="right" spinBox="true" caption="1dva, resolution 3.00Å" /> '''CRYSTAL STRUCTURE O... |
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[[Image:1dva.gif|left|200px]]<br /> | [[Image:1dva.gif|left|200px]]<br /><applet load="1dva" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="1dva" size=" | |||
caption="1dva, resolution 3.00Å" /> | caption="1dva, resolution 3.00Å" /> | ||
'''CRYSTAL STRUCTURE OF THE COMPLEX BETWEEN THE PEPTIDE EXOSITE INHIBITOR E-76 AND COAGULATION FACTOR VIIA'''<br /> | '''CRYSTAL STRUCTURE OF THE COMPLEX BETWEEN THE PEPTIDE EXOSITE INHIBITOR E-76 AND COAGULATION FACTOR VIIA'''<br /> | ||
==Overview== | ==Overview== | ||
Potent anticoagulants have been derived by targeting the tissue | 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. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
1DVA 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 GLC, FUC, FUL, CA, CAC, ACE and CH2 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Coagulation_factor_VIIa Coagulation factor VIIa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.21 3.4.21.21] Full crystallographic information is available from [http:// | 1DVA 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=GLC:'>GLC</scene>, <scene name='pdbligand=FUC:'>FUC</scene>, <scene name='pdbligand=FUL:'>FUL</scene>, <scene name='pdbligand=CA:'>CA</scene>, <scene name='pdbligand=CAC:'>CAC</scene>, <scene name='pdbligand=ACE:'>ACE</scene> and <scene name='pdbligand=CH2:'>CH2</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Coagulation_factor_VIIa Coagulation factor VIIa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.21 3.4.21.21] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1DVA OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Eigenbrot, C.]] | [[Category: Eigenbrot, C.]] | ||
[[Category: Ultsch, M | [[Category: Ultsch, M H.]] | ||
[[Category: ACE]] | [[Category: ACE]] | ||
[[Category: CA]] | [[Category: CA]] | ||
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[[Category: protein-peptide complex]] | [[Category: protein-peptide complex]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:20:50 2008'' | ||
