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1u9v
From Proteopedia
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|SITE= | |SITE= | ||
|LIGAND= <scene name='pdbligand=IHE:6-(CYCLOHEXYLAMINO)-9-[2-(4-METHYLPIPERAZIN-1-YL)-ETHYL]-9H-PURINE-2-CARBONITRILE'>IHE</scene> | |LIGAND= <scene name='pdbligand=IHE:6-(CYCLOHEXYLAMINO)-9-[2-(4-METHYLPIPERAZIN-1-YL)-ETHYL]-9H-PURINE-2-CARBONITRILE'>IHE</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] | + | |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> |
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1u9w|1U9W]], [[1u9x|1U9X]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1u9v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1u9v OCA], [http://www.ebi.ac.uk/pdbsum/1u9v PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1u9v RCSB]</span> | ||
}} | }} | ||
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==Overview== | ==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. | 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:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=601105 601105]] | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Cowan-Jacob, S W.]] | [[Category: Cowan-Jacob, S W.]] | ||
| - | [[Category: IHE]] | ||
[[Category: hydrolase]] | [[Category: hydrolase]] | ||
[[Category: sulfhydryl proteinase]] | [[Category: sulfhydryl proteinase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:07:21 2008'' |
Revision as of 21:07, 30 March 2008
| |||||||
| , resolution 2.2Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Activity: | Cathepsin K, with EC number 3.4.22.38 | ||||||
| Related: | 1U9W, 1U9X
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal Structure of the Cysteine Protease Human Cathepsin K in Complex with the Covalent Inhibitor NVP-ABE854
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.
About this Structure
1U9V 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 Mon Mar 31 00:07:21 2008
