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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
20
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pubmed:dateCreated |
2009-9-28
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pubmed:abstractText |
A pharmacophore mapping approach, derived from previous experience of PIKK family enzymes, was used to identify a hit series of selective inhibitors of the mammalian target of rapamycin (mTOR). Subsequent refinement of the SAR around this hit series based on a tri-substituted triazine scaffold has led to the discovery of potent and selective inhibitors of mTOR.
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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 |
Oct
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BaileyChristineC,
pubmed-author:BlackburnKristelK,
pubmed-author:CockcroftXiao-LingXL,
pubmed-author:EwenSallyS,
pubmed-author:FundoAlexandraA,
pubmed-author:GomezSylvieS,
pubmed-author:HermannGesineG,
pubmed-author:HicksonIanI,
pubmed-author:Le GallArmelleA,
pubmed-author:MalaguKarineK,
pubmed-author:MartinNiall M BNM,
pubmed-author:MenearKeith AKA,
pubmed-author:PikeKurt GKG,
pubmed-author:PresnotThomasT,
pubmed-author:SebastianLuisaL,
pubmed-author:SmithGraeme C MGC,
pubmed-author:SunoseMihiroM,
pubmed-author:TorodeEleanorE
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5898-901
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:19733066-Antineoplastic Agents,
pubmed-meshheading:19733066-Cell Line, Tumor,
pubmed-meshheading:19733066-Humans,
pubmed-meshheading:19733066-Morpholines,
pubmed-meshheading:19733066-Phosphatidylinositol 3-Kinases,
pubmed-meshheading:19733066-Protein Kinase Inhibitors,
pubmed-meshheading:19733066-Protein Kinases,
pubmed-meshheading:19733066-Pyrimidines,
pubmed-meshheading:19733066-Structure-Activity Relationship,
pubmed-meshheading:19733066-TOR Serine-Threonine Kinases,
pubmed-meshheading:19733066-Triazines
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pubmed:year |
2009
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pubmed:articleTitle |
Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.
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pubmed:affiliation |
KuDOS Pharmaceuticals Ltd, 410 Cambridge Science Park, Milton Road, Cambridge CB4 0PE, UK.
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pubmed:publicationType |
Journal Article
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