1snk
From Proteopedia
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[[Image:1snk.gif|left|200px]] | [[Image:1snk.gif|left|200px]] | ||
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'''Cathepsin K complexed with carbamate derivatized norleucine aldehyde''' | '''Cathepsin K complexed with carbamate derivatized norleucine aldehyde''' | ||
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[[Category: Thompson, J B.]] | [[Category: Thompson, J B.]] | ||
[[Category: Wright, L L.]] | [[Category: Wright, L L.]] | ||
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Revision as of 05:55, 3 May 2008
Cathepsin K complexed with carbamate derivatized norleucine aldehyde
Overview
The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S2 and S3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P2 and P3 positions afforded analogs with cathepsin K IC50s between 600 nM and 130 pM.
About this Structure
1SNK is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors., Boros EE, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Paulick MG, Shewchuk LM, Thompson JB, Willard DH Jr, Wright LL, Bioorg Med Chem Lett. 2004 Jul 5;14(13):3425-9. PMID:15177446 Page seeded by OCA on Sat May 3 08:55:25 2008