1q6k

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PDB ID 1q6k

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, resolution 2.1Å
Ligands: ,
Gene: CTSK OR CTSO (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 t-butyl(1S)-1-cyclohexyl-2-oxoethylcarbamate


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.

About this Structure

1Q6K is a Single protein structure of sequence from Homo sapiens. 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

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