1yk8

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[[Image:1yk8.gif|left|200px]]<br /><applet load="1yk8" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1yk8.gif|left|200px]]
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caption="1yk8, resolution 2.6&Aring;" />
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'''Cathepsin K complexed with a cyanamide-based inhibitor'''<br />
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{{Structure
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|PDB= 1yk8 |SIZE=350|CAPTION= <scene name='initialview01'>1yk8</scene>, resolution 2.6&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=T2M:TERT-BUTYL 2-CYANO-2-METHYLHYDRAZINECARBOXYLATE'>T2M</scene>
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|ACTIVITY= [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]
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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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'''Cathepsin K complexed with a cyanamide-based inhibitor'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1YK8 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=T2M:'>T2M</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1YK8 OCA].
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1YK8 is a [[Single protein]] structure of 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=1YK8 OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15896958 15896958]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/15896958 15896958]
[[Category: Cathepsin K]]
[[Category: Cathepsin K]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: protease]]
[[Category: protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:06:15 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:23:57 2008''

Revision as of 13:23, 20 March 2008

Image:1yk8.gif


PDB ID 1yk8

Drag the structure with the mouse to rotate
, resolution 2.6Å
Ligands:
Gene: CTSK, CTSO, CTSO2 (Homo sapiens)
Activity: Cathepsin K, with EC number 3.4.22.38
Coordinates: save as pdb, mmCIF, xml



Cathepsin K complexed with a cyanamide-based inhibitor


Contents

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.

Disease

Known disease associated with this structure: Pycnodysostosis OMIM:[601105]

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 Thu Mar 20 15:23:57 2008

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OCA

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