1u9x

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[[Image:1u9x.gif|left|200px]]<br /><applet load="1u9x" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1u9x.gif|left|200px]]
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caption="1u9x, resolution 2.1&Aring;" />
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'''Crystal Structure of the Cysteine Protease Human Cathepsin K in Complex with the Covalent Inhibitor NVP-ABJ688'''<br />
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{{Structure
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|PDB= 1u9x |SIZE=350|CAPTION= <scene name='initialview01'>1u9x</scene>, resolution 2.1&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=IHJ:9-CYCLOPENTYL-6-{2-[3-(4-METHYL-PIPERAZIN-1-YL)-PROPOXY]-PHENYLAMINO}-9H-PURINE-2-CARBONITRILE'>IHJ</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=
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}}
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'''Crystal Structure of the Cysteine Protease Human Cathepsin K in Complex with the Covalent Inhibitor NVP-ABJ688'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1U9X 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=IHJ:'>IHJ</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=1U9X OCA].
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1U9X 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=1U9X OCA].
==Reference==
==Reference==
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Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K., Altmann E, Cowan-Jacob SW, Missbach M, J Med Chem. 2004 Nov 18;47(24):5833-6. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15537340 15537340]
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Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K., Altmann E, Cowan-Jacob SW, Missbach M, J Med Chem. 2004 Nov 18;47(24):5833-6. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15537340 15537340]
[[Category: Cathepsin K]]
[[Category: Cathepsin K]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: sulfhydryl proteinase]]
[[Category: sulfhydryl proteinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:22:09 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:29:11 2008''

Revision as of 12:29, 20 March 2008

Image:1u9x.gif


PDB ID 1u9x

Drag the structure with the mouse to rotate
, resolution 2.1Å
Ligands:
Activity: Cathepsin K, with EC number 3.4.22.38
Coordinates: save as pdb, mmCIF, xml



Crystal Structure of the Cysteine Protease Human Cathepsin K in Complex with the Covalent Inhibitor NVP-ABJ688


Contents

Overview

Starting from the high-throughput screening hit 1a, novel cathepsin K inhibitors have been developed based on a purine scaffold. High-resolution X-ray structures of several derivatives have revealed the binding mode of these unique cysteine protease inhibitors.

Disease

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

About this Structure

1U9X is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K., Altmann E, Cowan-Jacob SW, Missbach M, J Med Chem. 2004 Nov 18;47(24):5833-6. PMID:15537340

Page seeded by OCA on Thu Mar 20 14:29:11 2008

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