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2bdl
From Proteopedia
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[[Image:2bdl.gif|left|200px]] | [[Image:2bdl.gif|left|200px]] | ||
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'''Cathepsin K complexed with a pyrrolidine ketoamide-based inhibitor''' | '''Cathepsin K complexed with a pyrrolidine ketoamide-based inhibitor''' | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Shewchuk, L M.]] | [[Category: Shewchuk, L M.]] | ||
| - | [[Category: | + | [[Category: Cathepsin]] |
| - | [[Category: | + | [[Category: Catk]] |
| - | [[Category: | + | [[Category: Cato]] |
| - | [[Category: | + | [[Category: Cysteine protease]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:08:40 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 17:08, 3 May 2008
Cathepsin K complexed with a pyrrolidine ketoamide-based inhibitor
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.
About this Structure
2BDL is a Single protein structure of sequence from Homo sapiens. 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 Sat May 3 20:08:40 2008
