1yk8

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[[Image:1yk8.gif|left|200px]]
[[Image:1yk8.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1yk8 |SIZE=350|CAPTION= <scene name='initialview01'>1yk8</scene>, resolution 2.6&Aring;
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The line below this paragraph, containing "STRUCTURE_1yk8", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=T2M:TERT-BUTYL+2-CYANO-2-METHYLHYDRAZINECARBOXYLATE'>T2M</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Cathepsin_K Cathepsin K], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.38 3.4.22.38] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= CTSK, CTSO, CTSO2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1yk8| PDB=1yk8 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yk8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yk8 OCA], [http://www.ebi.ac.uk/pdbsum/1yk8 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1yk8 RCSB]</span>
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}}
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'''Cathepsin K complexed with a cyanamide-based inhibitor'''
'''Cathepsin K complexed with a cyanamide-based inhibitor'''
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[[Category: Willard, D H.]]
[[Category: Willard, D H.]]
[[Category: Wright, L L.]]
[[Category: Wright, L L.]]
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[[Category: cathepsin]]
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[[Category: Cathepsin]]
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[[Category: catk]]
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[[Category: Catk]]
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[[Category: cysteine]]
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[[Category: Cysteine]]
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[[Category: protease]]
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[[Category: Protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:25:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:10:33 2008''
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Revision as of 13:25, 3 May 2008

Template:STRUCTURE 1yk8

Cathepsin K complexed with a cyanamide-based inhibitor


Overview

Conversion of the proline-derived cyanamide lead to an acyclic cyanamide capable of forming an additional hydrogen bond with cathepsin K resulted in a large increase in inhibitory activity. An X-ray structure of a co-crystal of a cyanamide with cathepsin K confirmed the enzyme interaction. Furthermore, a representative acyclic cyanamide inhibitor 6r was able to attenuate bone resorption in the rat calvarial model.

About this Structure

1YK8 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Acyclic cyanamide-based inhibitors of cathepsin K., Barrett DG, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Payne JA, Shewchuk LM, Willard DH Jr, Wright LL, Bioorg Med Chem Lett. 2005 Jun 15;15(12):3039-43. PMID:15896958 Page seeded by OCA on Sat May 3 16:25:30 2008

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