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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2006-2-27
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pubmed:abstractText |
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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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BlackW CameronWC,
pubmed-author:DeschenesDenisD,
pubmed-author:DesmaraisSylvieS,
pubmed-author:FalgueyretJean-PierreJP,
pubmed-author:GauthierJacques YvesJY,
pubmed-author:KimmelDonald BDB,
pubmed-author:LégerSergeS,
pubmed-author:LiChun SingCS,
pubmed-author:MasséFrédéricF,
pubmed-author:McGrathMary EME,
pubmed-author:McKayDaniel JDJ,
pubmed-author:PercivalM DavidMD,
pubmed-author:RiendeauDenisD,
pubmed-author:RodanSevgi BSB,
pubmed-author:ThérienMichelM,
pubmed-author:TruongVouy-LinhVL,
pubmed-author:WesolowskiGreggG,
pubmed-author:ZamboniRobertR
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pubmed:issnType |
Print
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|
pubmed:day |
1
|
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pubmed:volume |
16
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pubmed:owner |
NLM
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|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
1985-9
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:16413777-Animals,
pubmed-meshheading:16413777-Cathepsin K,
pubmed-meshheading:16413777-Cathepsins,
pubmed-meshheading:16413777-Crystallography, X-Ray,
pubmed-meshheading:16413777-Cysteine Proteinase Inhibitors,
pubmed-meshheading:16413777-Female,
pubmed-meshheading:16413777-Macaca mulatta,
pubmed-meshheading:16413777-Models, Molecular,
pubmed-meshheading:16413777-Ovariectomy
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pubmed:year |
2006
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pubmed:articleTitle |
Identification of a potent and selective non-basic cathepsin K inhibitor.
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pubmed:affiliation |
Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe-Claire-Dorval, Que., Canada H9R 4P8. chunsing_li@merck.com
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pubmed:publicationType |
Journal Article
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