1snk
From Proteopedia
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| , resolution 2.40Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | and | ||||||
| Gene: | CTSK, CTSO, CTSO2 (Homo sapiens) | ||||||
| Activity: | Cathepsin K, with EC number 3.4.22.38 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Cathepsin K complexed with carbamate derivatized norleucine aldehyde
Contents |
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.
Disease
Known disease associated with this structure: Pycnodysostosis OMIM:[601105]
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 Thu Mar 20 14:07:18 2008
Categories: Cathepsin K | Homo sapiens | Single protein | Boros, E E. | Deaton, D N. | Hassell, A M. | Jr., D H.Willard. | McFadyen, R B. | Miller, A B. | Miller, L R. | Shewchuk, L M. | Thompson, J B. | Wright, L L. | MYE | SO4 | Catk
