1yk8: Difference between revisions
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New page: left|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'' | ||
