1snk
From Proteopedia
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| , resolution 2.40Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , | ||||||
| Gene: | CTSK, CTSO, CTSO2 (Homo sapiens) | ||||||
| Activity: | Cathepsin K, with EC number 3.4.22.38 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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 Sun Mar 30 23:44:31 2008
