4omd

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{{STRUCTURE_4omd| PDB=4omd | SCENE= }}
 
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===X-ray structure of human furin in complex with the competitive inhibitor Phac-RVR-Amba===
 
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{{ABSTRACT_PUBMED_24666235}}
 
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==Function==
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==X-ray structure of human furin in complex with the competitive inhibitor Phac-RVR-Amba==
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[[http://www.uniprot.org/uniprot/FURIN_HUMAN FURIN_HUMAN]] Furin is likely to represent the ubiquitous endoprotease activity within constitutive secretory pathways and capable of cleavage at the RX(K/R)R consensus motif.<ref>PMID:7690548</ref>
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<StructureSection load='4omd' size='340' side='right'caption='[[4omd]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4omd]] is a 12 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4OMD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4OMD FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.7&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=00S:4-(AMINOMETHYL)BENZENECARBOXIMIDAMIDE'>00S</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=HY1:PHENYLACETALDEHYDE'>HY1</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4omd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4omd OCA], [https://pdbe.org/4omd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4omd RCSB], [https://www.ebi.ac.uk/pdbsum/4omd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4omd ProSAT]</span></td></tr>
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</table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Furin inhibitors are promising therapeutics for the treatment of cancer and numerous infections caused by bacteria and viruses, including the highly lethal Bacillus anthracis or the pandemic influenza virus. Development and improvement of inhibitors for pharmacological use require a detailed knowledge of the protease's substrate and inhibitor binding properties. Here we present a novel preparation of human furin and the first crystal structures of this enzyme in complex with noncovalent inhibitors. We show the inhibitor exchange by soaking, allowing the investigation of additional inhibitors and substrate analogues. Thus, our work provides a basis for the rational design of furin inhibitors.
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==About this Structure==
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X-ray Structures of Human Furin in Complex with Competitive Inhibitors.,Dahms SO, Hardes K, Becker GL, Steinmetzer T, Brandstetter H, Than ME ACS Chem Biol. 2014 Apr 1. PMID:24666235<ref>PMID:24666235</ref>
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[[4omd]] is a 12 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4OMD OCA].
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==Reference==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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<ref group="xtra">PMID:024666235</ref><references group="xtra"/><references/>
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</div>
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[[Category: Furin]]
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<div class="pdbe-citations 4omd" style="background-color:#fffaf0;"></div>
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[[Category: Dahms, S O.]]
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== References ==
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[[Category: Than, M E.]]
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<references/>
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[[Category: Competitive inhibitor]]
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__TOC__
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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</StructureSection>
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[[Category: Pro-protein convertase]]
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[[Category: Homo sapiens]]
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[[Category: Protease-inhibitor complex]]
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[[Category: Large Structures]]
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[[Category: Serine protease]]
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[[Category: Dahms SO]]
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[[Category: Than ME]]

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X-ray structure of human furin in complex with the competitive inhibitor Phac-RVR-Amba

PDB ID 4omd

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