4aig: Difference between revisions
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New page: left|200px<br /><applet load="4aig" size="450" color="white" frame="true" align="right" spinBox="true" caption="4aig, resolution 2.00Å" /> '''ADAMALYSIN II WITH P... |
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[[Image:4aig.gif|left|200px]]<br /><applet load="4aig" size=" | [[Image:4aig.gif|left|200px]]<br /><applet load="4aig" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="4aig, resolution 2.00Å" /> | caption="4aig, resolution 2.00Å" /> | ||
'''ADAMALYSIN II WITH PHOSPHONATE INHIBITOR'''<br /> | '''ADAMALYSIN II WITH PHOSPHONATE INHIBITOR'''<br /> | ||
==Overview== | ==Overview== | ||
The search of reprolysin inhibitors offers the possibility of intervention | The search of reprolysin inhibitors offers the possibility of intervention against both matrixins and ADAMs. Here we report the crystal structure of the complex between adamalysin II, a member of the reprolysin family, and a phosphonate inhibitor modeled on an endogenous venom tripeptide. The inhibitor occupies the primed region of the cleavage site adopting a retro-binding mode. The phosphonate group ligates the zinc ion in an asymmetric bidentate mode and the adjacent Trp indole system partly fills the primary specificity subsite S1'. An adamalysin-based model of tumor necrosis factor-alpha-converting enzyme (TACE) reveals a smaller S1' pocket for this enzyme. | ||
==About this Structure== | ==About this Structure== | ||
4AIG is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Crotalus_adamanteus Crotalus adamanteus] with ZN, CA and FLX as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Adamalysin Adamalysin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.46 3.4.24.46] Full crystallographic information is available from [http:// | 4AIG is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Crotalus_adamanteus Crotalus adamanteus] with <scene name='pdbligand=ZN:'>ZN</scene>, <scene name='pdbligand=CA:'>CA</scene> and <scene name='pdbligand=FLX:'>FLX</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Adamalysin Adamalysin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.46 3.4.24.46] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AIG OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: zinc protease]] | [[Category: zinc protease]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 19:12:39 2008'' | ||
