1yk7

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[[Image:1yk7.png|left|200px]]
 
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==Cathepsin K complexed with a cyanopyrrolidine inhibitor==
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The line below this paragraph, containing "STRUCTURE_1yk7", creates the "Structure Box" on the page.
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<StructureSection load='1yk7' size='340' side='right'caption='[[1yk7]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[1yk7]] 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=1YK7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1YK7 FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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]] 2.5&#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=NBL:N2-[(BENZYLOXY)CARBONYL]-N1-[(3S)-1-CYANOPYRROLIDIN-3-YL]-L-LEUCINAMIDE'>NBL</scene></td></tr>
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{{STRUCTURE_1yk7| PDB=1yk7 | SCENE= }}
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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=1yk7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yk7 OCA], [https://pdbe.org/1yk7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1yk7 RCSB], [https://www.ebi.ac.uk/pdbsum/1yk7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1yk7 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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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/yk/1yk7_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1yk7 ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Starting from a PDE IV inhibitor hit derived from high throughput screening of the compound collection, a key pyrrolidine cyanamide pharmacophore was identified. Modifications of the pyrrolidine ring produced enhancements in cathepsin K inhibition. An X-ray co-crystal structure of a cyanamide with cathepsin K confirmed the mode of inhibition.
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===Cathepsin K complexed with a cyanopyrrolidine inhibitor===
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Novel and potent cyclic cyanamide-based cathepsin K inhibitors.,Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Shewchuk LM, Tavares FX, Willard DH Jr, Wright LL Bioorg Med Chem Lett. 2005 Apr 1;15(7):1815-9. PMID:15780613<ref>PMID:15780613</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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The line below this paragraph, {{ABSTRACT_PUBMED_15780613}}, adds the Publication Abstract to the page
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<div class="pdbe-citations 1yk7" style="background-color:#fffaf0;"></div>
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(as it appears on PubMed at http://www.pubmed.gov), where 15780613 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15780613}}
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==About this Structure==
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[[1yk7]] is a 1 chain structure of [[Cathepsin]] 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=1YK7 OCA].
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==See Also==
==See Also==
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*[[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:15780613</ref><references group="xtra"/>
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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: Barrett, D G.]]
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[[Category: Large Structures]]
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[[Category: Deaton, D N.]]
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[[Category: Barrett DG]]
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[[Category: Hassell, A M.]]
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[[Category: Deaton DN]]
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[[Category: McFadyen, R B.]]
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[[Category: Hassell AM]]
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[[Category: Miller, A B.]]
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[[Category: McFadyen RB]]
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[[Category: Miller, L R.]]
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[[Category: Miller AB]]
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[[Category: Shewchuk, L M.]]
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[[Category: Miller LR]]
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[[Category: Tavares, F X.]]
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[[Category: Shewchuk LM]]
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[[Category: Willard, D H.]]
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[[Category: Tavares FX]]
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[[Category: Wright, L L.]]
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[[Category: Willard DH]]
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[[Category: Cathepsin]]
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[[Category: Wright LL]]
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[[Category: Catk]]
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[[Category: Cysteine]]
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[[Category: Hydrolase]]
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[[Category: Protease]]
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Current revision

Cathepsin K complexed with a cyanopyrrolidine inhibitor

PDB ID 1yk7

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