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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2010-4-5
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pubmed:abstractText |
A novel series of tricyclic gamma-secretase inhibitors was designed and synthesized via a conformational analysis of literature compounds. The preliminary results have shown that compounds in this new series have much improved in vitro potency and in vivo profiles. More importantly, they have greatly reduced Notch related toxicity that was associated with previous gamma-secretase 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 |
1464-3405
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pubmed:author |
pubmed-author:AbbeS ESE,
pubmed-author:AsberomTedT,
pubmed-author:BennettChadC,
pubmed-author:BurnettDuane ADA,
pubmed-author:CladerJohnJ,
pubmed-author:ColeDavidD,
pubmed-author:DomalskiMartinM,
pubmed-author:GreenleeWilliamW,
pubmed-author:HydeLynnL,
pubmed-author:JosienHubertH,
pubmed-author:LiHongmeiH,
pubmed-author:LiQiangQ,
pubmed-author:McBriarMarkM,
pubmed-author:McKittrickBrianB,
pubmed-author:McPhailAndrew TAT,
pubmed-author:PissarnitskiDmitriD,
pubmed-author:RajagopalanMuraliM,
pubmed-author:SasikumarThavalakulamgarT,
pubmed-author:SuJingJ,
pubmed-author:TangHaiqunH,
pubmed-author:TowMM,
pubmed-author:WuWen-LianWL,
pubmed-author:ZhangLiliL,
pubmed-author:ZhaoZhiqiangZ
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2591-6
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pubmed:meshHeading |
pubmed-meshheading:20236824-Amyloid Precursor Protein Secretases,
pubmed-meshheading:20236824-Animals,
pubmed-meshheading:20236824-Crystallography, X-Ray,
pubmed-meshheading:20236824-Drug Design,
pubmed-meshheading:20236824-Mice,
pubmed-meshheading:20236824-Models, Molecular,
pubmed-meshheading:20236824-Receptors, Notch,
pubmed-meshheading:20236824-Sulfones
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pubmed:year |
2010
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pubmed:articleTitle |
Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.
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pubmed:affiliation |
Merck Research Laboratories, Kenilworth, NJ 07033, USA. ruo.xu@merck.com
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pubmed:publicationType |
Journal Article
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