2bdl: Difference between revisions
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New page: left|200px<br /> <applet load="2bdl" size="450" color="white" frame="true" align="right" spinBox="true" caption="2bdl, resolution 2.0Å" /> '''Cathepsin K complexe... |
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[[Image:2bdl.gif|left|200px]]<br /> | [[Image:2bdl.gif|left|200px]]<br /><applet load="2bdl" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2bdl" size=" | |||
caption="2bdl, resolution 2.0Å" /> | caption="2bdl, resolution 2.0Å" /> | ||
'''Cathepsin K complexed with a pyrrolidine ketoamide-based inhibitor'''<br /> | '''Cathepsin K complexed with a pyrrolidine ketoamide-based inhibitor'''<br /> | ||
==Overview== | ==Overview== | ||
Starting from a potent pantolactone ketoamide cathepsin K inhibitor | Starting from a potent pantolactone ketoamide cathepsin K inhibitor discovered from structural screening, conversion of the lactone scaffold to a pyrrolidine scaffold allowed exploration of the S(3) subsite of cathepsin K. Manipulation of P3 and P1' groups afforded potent inhibitors with drug-like properties. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
2BDL 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 4PR 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:// | 2BDL 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=4PR:'>4PR</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=2BDL OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Shewchuk, L | [[Category: Shewchuk, L M.]] | ||
[[Category: 4PR]] | [[Category: 4PR]] | ||
[[Category: cathepsin]] | [[Category: cathepsin]] | ||
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[[Category: cysteine protease]] | [[Category: cysteine protease]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:36:40 2008'' | ||
