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1q6k

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(New page: 200px<br /> <applet load="1q6k" size="450" color="white" frame="true" align="right" spinBox="true" caption="1q6k, resolution 2.1&Aring;" /> '''Cathepsin K complexe...)
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Revision as of 16:44, 12 November 2007

Image:1q6k.gif

1q6k, resolution 2.1Å

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Cathepsin K complexed with t-butyl(1S)-1-cyclohexyl-2-oxoethylcarbamate

Contents

Overview

The synthesis and biological activity of a series of aldehyde inhibitors, of cathepsin K are reported. Exploration of the properties of the S(1), subsite with a series of alpha-amino aldehyde derivatives substituted at, the P(1) position afforded compounds with cathepsin K IC(50)s between 52, microM and 15 nM.

Disease

Known disease associated with this structure: Pycnodysostosis OMIM:[601105]

About this Structure

1Q6K is a Single protein structure of sequence from Homo sapiens with SO4 and TCO as ligands. Active as Cathepsin K, with EC number 3.4.22.38 Full crystallographic information is available from OCA.

Reference

Exploration of the P1 SAR of aldehyde cathepsin K inhibitors., Catalano JG, Deaton DN, Furfine ES, Hassell AM, McFadyen RB, Miller AB, Miller LR, Shewchuk LM, Willard DH Jr, Wright LL, Bioorg Med Chem Lett. 2004 Jan 5;14(1):275-8. PMID:14684342

Page seeded by OCA on Mon Nov 12 18:50:57 2007

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