1vsn

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{{STRUCTURE_1vsn| PDB=1vsn | SCENE= }}
{{STRUCTURE_1vsn| PDB=1vsn | SCENE= }}
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'''Crystal structure of a potent small molecule inhibitor bound to cathepsin K'''
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===Crystal structure of a potent small molecule inhibitor bound to cathepsin K===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 16413777 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16413777}}
==About this Structure==
==About this Structure==
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[[Category: Proteae]]
[[Category: Proteae]]
[[Category: Structure-guided drug design]]
[[Category: Structure-guided drug design]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 12:52:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 07:00:24 2008''

Revision as of 04:00, 28 July 2008

Image:1vsn.png

Template:STRUCTURE 1vsn

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

Template:ABSTRACT PUBMED 16413777

About this Structure

1VSN is a Single protein structure of sequence from Homo sapiens. This structure supersedes the now removed PDB entry 2fdz. 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

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