1u9w: Difference between revisions
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'''Crystal Structure of the Cysteine Protease Human Cathepsin K in Complex with the Covalent Inhibitor NVP-ABI491''' | {{Structure | ||
|PDB= 1u9w |SIZE=350|CAPTION= <scene name='initialview01'>1u9w</scene>, resolution 2.3Å | |||
|SITE= | |||
|LIGAND= <scene name='pdbligand=IHI:9-CYCLOPENTYL-6-[2-(3-IMIDAZOL-1-YL-PROPOXY)-PHENYLAMINO]-9H-PURINE-2-CARBONITRILE'>IHI</scene> | |||
|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] | |||
|GENE= | |||
}} | |||
'''Crystal Structure of the Cysteine Protease Human Cathepsin K in Complex with the Covalent Inhibitor NVP-ABI491''' | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
1U9W is a [ | 1U9W 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=1U9W OCA]. | ||
==Reference== | ==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:[http:// | 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]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:29:16 2008'' | ||
Revision as of 12:29, 20 March 2008
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| 1u9w, resolution 2.3Å | |||||||||||||
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| Ligands: | IHI | ||||||||||||
| 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-ABI491
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
1U9W 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
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