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2bdl
From Proteopedia
(New page: 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'' |
Revision as of 14:36, 21 February 2008
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Cathepsin K complexed with a pyrrolidine ketoamide-based inhibitor
Contents |
Overview
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
Known disease associated with this structure: Pycnodysostosis OMIM:[601105]
About this Structure
2BDL 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
Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors., Barrett DG, Catalano JG, Deaton DN, Hassell AM, Long ST, Miller AB, Miller LR, Ray JA, Samano V, Shewchuk LM, Wells-Knecht KJ, Willard DH Jr, Wright LL, Bioorg Med Chem Lett. 2006 Mar 15;16(6):1735-9. Epub 2006 Jan 11. PMID:16376075
Page seeded by OCA on Thu Feb 21 16:36:40 2008
Categories: Cathepsin K | Homo sapiens | Single protein | Shewchuk, L M. | 4PR | Cathepsin | Catk | Cato | Cysteine protease
