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6qbs
From Proteopedia
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==The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K== | ==The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K== | ||
| - | <StructureSection load='6qbs' size='340' side='right' | + | <StructureSection load='6qbs' size='340' side='right'caption='[[6qbs]], [[Resolution|resolution]] 1.70Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[6qbs]] is a 2 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[6qbs]] is a 2 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=6QBS OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6QBS FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=HVW:(2~{S})-4-methyl-~{N}-prop-2-enyl-2-[[(1~{S})-2,2,2-tris(fluoranyl)-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide'>HVW</scene | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.7Å</td></tr> |
| - | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=HVW:(2~{S})-4-methyl-~{N}-prop-2-enyl-2-[[(1~{S})-2,2,2-tris(fluoranyl)-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide'>HVW</scene></td></tr> | |
| - | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6qbs FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6qbs OCA], [https://pdbe.org/6qbs PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6qbs RCSB], [https://www.ebi.ac.uk/pdbsum/6qbs PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6qbs ProSAT]</span></td></tr> | |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | |
</table> | </table> | ||
== Disease == | == Disease == | ||
| - | [ | + | [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> |
== Function == | == Function == | ||
| - | [ | + | [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. |
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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</div> | </div> | ||
<div class="pdbe-citations 6qbs" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 6qbs" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[Cathepsin 3D structures|Cathepsin 3D structures]] | ||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: | + | [[Category: Large Structures]] |
| - | + | [[Category: Hermans J]] | |
| - | + | [[Category: Jansen IDC]] | |
| - | [[Category: Hermans | + | [[Category: Loboda J]] |
| - | [[Category: Jansen | + | [[Category: Mons E]] |
| - | [[Category: Loboda | + | [[Category: Ovaa H]] |
| - | [[Category: Mons | + | [[Category: Turk B]] |
| - | [[Category: Ovaa | + | [[Category: Turk D]] |
| - | [[Category: Turk | + | [[Category: Verdoes M]] |
| - | [[Category: Turk | + | [[Category: Van Boeckel CAA]] |
| - | + | [[Category: Van Doodewaerd BR]] | |
| - | [[Category: Verdoes | + | [[Category: Van Veelen PA]] |
| - | [[Category: | + | |
| - | [[Category: | + | |
| - | [[Category: | + | |
Current revision
The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K
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Categories: Homo sapiens | Large Structures | Hermans J | Jansen IDC | Loboda J | Mons E | Ovaa H | Turk B | Turk D | Verdoes M | Van Boeckel CAA | Van Doodewaerd BR | Van Veelen PA
