1vsn

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spinqualitylabelsall models 1vsn, resolution 2.000Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Crystal structure of a potent small molecule inhibitor bound to cathepsin K

Contents 1 Overview 2 Disease 3 About this Structure 4 Reference

Overview

Based on our previous study with trifluoroethylamine as a P2-P3 amide, isostere of cathepsin K inhibitor, further optimization led to, identification of compound 22 (L-873724) as a potent and selective, non-basic cathepsin K inhibitor. This compound showed excellent, pharmacokinetics and efficacy in an ovariectomized (OVX) rhesus monkey, model. The volumes of distribution close to unity were consistent with, this compound not being lysosomotropic, which is a characteristic of basic, cathepsin K inhibitors.

Disease

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

About this Structure

1VSN is a Single protein structure of sequence from Homo sapiens with NFT as ligand. This structure superseeds the now removed PDB entry 2FDZ. Active as Cathepsin K, with EC number 3.4.22.38 Full crystallographic information is available from OCA.

Reference

Identification of a potent and selective non-basic cathepsin K inhibitor., Li CS, Deschenes D, Desmarais S, Falgueyret JP, Gauthier JY, Kimmel DB, Leger S, Masse F, McGrath ME, McKay DJ, Percival MD, Riendeau D, Rodan SB, Therien M, Truong VL, Wesolowski G, Zamboni R, Black WC, Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9. Epub 2006 Jan 18. PMID:16413777

Page seeded by OCA on Mon Nov 12 19:44:53 2007