1snk

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spinqualitylabelsall models 1snk, resolution 2.40Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Cathepsin K complexed with carbamate derivatized norleucine aldehyde

Contents 1 Overview 2 Disease 3 About this Structure 4 Reference

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 with SO4 and MYE as ligands. Active as Cathepsin K, with EC number 3.4.22.38 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 Mon Nov 12 19:15:41 2007