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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
21
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pubmed:dateCreated |
2005-9-26
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pubmed:abstractText |
The P2-P3 amide of dipeptide cathepsin K inhibitors can be replaced by the metabolically stable trifluoroethylamine group. The non-basic nature of the nitrogen allows the important hydrogen bond to Gly66 to be made. The resulting compounds are 10- to 20-fold more potent than the corresponding amide derivatives. Compound 8 is a 5 pM inhibitor of human cathepsin K with >10,000-fold selectivity over other cathepsins.
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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 |
Nov
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BaylyChristopher ICI,
pubmed-author:BlackW CameronWC,
pubmed-author:DavisDana EDE,
pubmed-author:DesmaraisSylvieS,
pubmed-author:FalgueyretJean-PierreJP,
pubmed-author:LégerSergeS,
pubmed-author:LiChun SingCS,
pubmed-author:MasséFrédéricF,
pubmed-author:McKayDaniel JDJ,
pubmed-author:PalmerJames TJT,
pubmed-author:PercivalM DavidMD,
pubmed-author:RobichaudJoëlJ,
pubmed-author:TsouNancyN,
pubmed-author:ZamboniRobertR
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4741-4
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
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pubmed:year |
2005
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pubmed:articleTitle |
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
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pubmed:affiliation |
Merck Frosst Centre for Therapeutic Research, P.O. Box 1005, Pointe-Claire-Dorval, Que., Canada H9R 4P8. blackc@merck.com
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pubmed:publicationType |
Journal Article
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