3ovz

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{{STRUCTURE_3ovz| PDB=3ovz | SCENE= }}
 
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===Cathepsin K in complex with a covalent inhibitor with a ketoamide warhead===
 
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{{ABSTRACT_PUBMED_21030256}}
 
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==Disease==
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==Cathepsin K in complex with a covalent inhibitor with a ketoamide warhead==
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[[http://www.uniprot.org/uniprot/CATK_HUMAN CATK_HUMAN]] Defects in CTSK are the cause of pycnodysostosis (PKND) [MIM:[http://omim.org/entry/265800 265800]]. PKND is an autosomal recessive osteochondrodysplasia characterized by osteosclerosis and short stature.<ref>PMID:8703060</ref><ref>PMID:9529353</ref><ref>PMID:10491211</ref><ref>PMID:10878663</ref>
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<StructureSection load='3ovz' size='340' side='right'caption='[[3ovz]], [[Resolution|resolution]] 2.02&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3ovz]] is a 1 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=3OVZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3OVZ 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]] 2.02&#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=O96:N-[(1S)-3-AMINO-1-ETHYL-2,3-DIOXOPROPYL]-2-CHLORO-4-(PYRIDIN-2-YLMETHOXY)-3-(TRIFLUOROMETHYL)BENZAMIDE'>O96</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=3ovz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ovz OCA], [https://pdbe.org/3ovz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3ovz RCSB], [https://www.ebi.ac.uk/pdbsum/3ovz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3ovz ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/CATK_HUMAN CATK_HUMAN] Defects in CTSK are the cause of pycnodysostosis (PKND) [MIM:[https://omim.org/entry/265800 265800]. PKND is an autosomal recessive osteochondrodysplasia characterized by osteosclerosis and short stature.<ref>PMID:8703060</ref> <ref>PMID:9529353</ref> <ref>PMID:10491211</ref> <ref>PMID:10878663</ref>
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== Function ==
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[https://www.uniprot.org/uniprot/CATK_HUMAN CATK_HUMAN] Closely involved in osteoclastic bone resorption and may participate partially in the disorder of bone remodeling. Displays potent endoprotease activity against fibrinogen at acid pH. May play an important role in extracellular matrix degradation.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The trifluoromethylphenyl P2 motif from previously reported heteroarylnitrile series has been successfully applied for the design and synthesis of highly potent novel ketoamide-based cathepsin S inhibitors. The key in this process is the change of the torsion angle between the P2 phenyl ring and the attached secondary amide by adding a small Cl, F, or Me group at the 2-position.
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==Function==
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Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.,Cai J, Robinson J, Belshaw S, Everett K, Fradera X, van Zeeland M, van Berkom L, van Rijnsbergen P, Popplestone L, Baugh M, Dempster M, Bruin J, Hamilton W, Kinghorn E, Westwood P, Kerr J, Rankovic Z, Arbuckle W, Bennett DJ, Jones PS, Long C, Martin I, Uitdehaag JC, Meulemans T Bioorg Med Chem Lett. 2010 Dec 1;20(23):6890-4. Epub 2010 Oct 26. PMID:21030256<ref>PMID:21030256</ref>
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[[http://www.uniprot.org/uniprot/CATK_HUMAN CATK_HUMAN]] Closely involved in osteoclastic bone resorption and may participate partially in the disorder of bone remodeling. Displays potent endoprotease activity against fibrinogen at acid pH. May play an important role in extracellular matrix degradation.
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==About this Structure==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[3ovz]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3OVZ OCA].
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</div>
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<div class="pdbe-citations 3ovz" style="background-color:#fffaf0;"></div>
==See Also==
==See Also==
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*[[Cathepsin|Cathepsin]]
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*[[Cathepsin 3D structures|Cathepsin 3D structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:021030256</ref><references group="xtra"/><references/>
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__TOC__
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[[Category: Cathepsin K]]
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Fradera, X.]]
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[[Category: Large Structures]]
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[[Category: Uitdehaag, J C.M.]]
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[[Category: Fradera X]]
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[[Category: Zeeland, M van.]]
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[[Category: Uitdehaag JCM]]
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[[Category: Cathepsin k]]
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[[Category: Van Zeeland M]]
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[[Category: Covalent inhibitor]]
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[[Category: Hydrolase]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Ketoamide warhead]]
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[[Category: Ligand forms covalent bond to cys25]]
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[[Category: Lysosome]]
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Current revision

Cathepsin K in complex with a covalent inhibitor with a ketoamide warhead

PDB ID 3ovz

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