1u9v

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(New page: 200px<br /> <applet load="1u9v" size="450" color="white" frame="true" align="right" spinBox="true" caption="1u9v, resolution 2.2&Aring;" /> '''Crystal Structure of...)
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[[Image:1u9v.gif|left|200px]]<br />
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[[Image:1u9v.gif|left|200px]]<br /><applet load="1u9v" size="350" color="white" frame="true" align="right" spinBox="true"
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<applet load="1u9v" size="450" color="white" frame="true" align="right" spinBox="true"
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caption="1u9v, resolution 2.2&Aring;" />
caption="1u9v, resolution 2.2&Aring;" />
'''Crystal Structure of the Cysteine Protease Human Cathepsin K in Complex with the Covalent Inhibitor NVP-ABE854'''<br />
'''Crystal Structure of the Cysteine Protease Human Cathepsin K in Complex with the Covalent Inhibitor NVP-ABE854'''<br />
==Overview==
==Overview==
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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.
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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==
==Disease==
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==About this Structure==
==About this Structure==
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1U9V 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 IHE 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://ispc.weizmann.ac.il/oca-bin/ocashort?id=1U9V OCA].
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1U9V 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=IHE:'>IHE</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=1U9V OCA].
==Reference==
==Reference==
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Cowan-Jacob, S.W.]]
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[[Category: Cowan-Jacob, S W.]]
[[Category: IHE]]
[[Category: IHE]]
[[Category: hydrolase]]
[[Category: hydrolase]]
[[Category: sulfhydryl proteinase]]
[[Category: sulfhydryl proteinase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 19:32:48 2007''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:22:09 2008''

Revision as of 13:22, 21 February 2008


1u9v, resolution 2.2Å

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Crystal Structure of the Cysteine Protease Human Cathepsin K in Complex with the Covalent Inhibitor NVP-ABE854

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

1U9V is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Cathepsin K, with EC number 3.4.22.38 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 Feb 21 15:22:09 2008

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