1yk8
From Proteopedia
(New page: 200px<br /> <applet load="1yk8" size="450" color="white" frame="true" align="right" spinBox="true" caption="1yk8, resolution 2.6Å" /> '''Cathepsin K complexe...) |
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| - | [[Image:1yk8.gif|left|200px]]<br /> | + | [[Image:1yk8.gif|left|200px]]<br /><applet load="1yk8" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1yk8" size=" | + | |
caption="1yk8, resolution 2.6Å" /> | caption="1yk8, resolution 2.6Å" /> | ||
'''Cathepsin K complexed with a cyanamide-based inhibitor'''<br /> | '''Cathepsin K complexed with a cyanamide-based inhibitor'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Conversion of the proline-derived cyanamide lead to an acyclic cyanamide | + | 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== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 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 T2M 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:// | + | 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]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Barrett, D | + | [[Category: Barrett, D G.]] |
| - | [[Category: Deaton, D | + | [[Category: Deaton, D N.]] |
| - | [[Category: Hassell, A | + | [[Category: Hassell, A M.]] |
| - | [[Category: McFadyen, R | + | [[Category: McFadyen, R B.]] |
| - | [[Category: Miller, A | + | [[Category: Miller, A B.]] |
| - | [[Category: Miller, L | + | [[Category: Miller, L R.]] |
| - | [[Category: Payne, J | + | [[Category: Payne, J A.]] |
| - | [[Category: Shewchuk, L | + | [[Category: Shewchuk, L M.]] |
| - | [[Category: Willard, D | + | [[Category: Willard, D H.]] |
| - | [[Category: Wright, L | + | [[Category: Wright, L L.]] |
[[Category: T2M]] | [[Category: T2M]] | ||
[[Category: cathepsin]] | [[Category: cathepsin]] | ||
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[[Category: protease]] | [[Category: protease]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:06:15 2008'' |
Revision as of 14:06, 21 February 2008
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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 with as ligand. Active as Cathepsin K, with EC number 3.4.22.38 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 Feb 21 16:06:15 2008
Categories: Cathepsin K | Homo sapiens | Single protein | Barrett, D G. | Deaton, D N. | Hassell, A M. | McFadyen, R B. | Miller, A B. | Miller, L R. | Payne, J A. | Shewchuk, L M. | Willard, D H. | Wright, L L. | T2M | Cathepsin | Catk | Cysteine | Protease
