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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
2006-7-17
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pubmed:abstractText |
Novel 1-(2-acylhydrazinocarbonyl)cycloalkyl carboxamides were designed as peptidomimetic inhibitors of interleukin-1beta converting enzyme (ICE). A short synthesis was developed and moderately potent ICE inhibitors were identified (IC(50) values <100 nM). Most of the synthesized examples were selective for ICE versus the related cysteine proteases caspase-3 and caspase-8, although several dual-acting inhibitors of ICE and caspase-8 were identified. Several of the more potent ICE inhibitors were also shown to inhibit IL-1beta production in a whole cell assay (IC(50) < 500 nM).
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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 |
Aug
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:DeBiswanathB,
pubmed-author:DemuthThomas PTPJr,
pubmed-author:EllisChristopher DCD,
pubmed-author:FancherAmy NAN,
pubmed-author:LaufersweilerMichael CMC,
pubmed-author:O'NeilSteven VSV,
pubmed-author:OppongKofi AKA,
pubmed-author:ShevilleJustinJ,
pubmed-author:SoperDavid LDL,
pubmed-author:SuchanekMaureen KMK,
pubmed-author:WangRichard LRL,
pubmed-author:WangYiliY,
pubmed-author:WosJohn AJA,
pubmed-author:YenPP
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pubmed:issnType |
Print
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pubmed:day |
15
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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 |
4233-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16782334-Amides,
pubmed-meshheading:16782334-Aminoimidazole Carboxamide,
pubmed-meshheading:16782334-Caspase 1,
pubmed-meshheading:16782334-Caspase 8,
pubmed-meshheading:16782334-Caspases,
pubmed-meshheading:16782334-Chemistry, Pharmaceutical,
pubmed-meshheading:16782334-Cysteine Endopeptidases,
pubmed-meshheading:16782334-Drug Industry,
pubmed-meshheading:16782334-Drug Screening Assays, Antitumor,
pubmed-meshheading:16782334-Enzyme Inhibitors,
pubmed-meshheading:16782334-Humans,
pubmed-meshheading:16782334-Hydrazines,
pubmed-meshheading:16782334-Inhibitory Concentration 50,
pubmed-meshheading:16782334-Models, Chemical
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pubmed:year |
2006
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pubmed:articleTitle |
Synthesis and evaluation of novel 1-(2-acylhydrazinocarbonyl)-cycloalkyl carboxamides as interleukin-1beta converting enzyme (ICE) inhibitors.
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pubmed:affiliation |
Procter & Gamble Pharmaceuticals, Mason, OH 45040, USA.
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pubmed:publicationType |
Journal Article
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