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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
A series of (hetero)arylpyrimidines agonists of the Wnt-beta-catenin cellular messaging system have been prepared. These compounds show activity in U2OS cells transfected with Wnt-3a, TCF-luciferase, Dkk-1 and tk-Renilla. Selected compounds show minimal GSK-3beta inhibition indicating that the Wnt-beta-catenin agonism activity most likely comes from interaction at Wnt-3a/Dkk-1. Two examples 1 and 25 show in vivo osteogenic activity in a mouse calvaria model. One example 1 is shown to activate non-phosphorylated beta-catenin formation in bone.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/DKK1 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Glycogen Synthase Kinase 3,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Intercellular Signaling Peptides...,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Fusion Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/WNT3A protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Wnt Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Wnt3 Protein,
http://linkedlifedata.com/resource/pubmed/chemical/Wnt3A Protein,
http://linkedlifedata.com/resource/pubmed/chemical/Wnt3a protein, mouse,
http://linkedlifedata.com/resource/pubmed/chemical/beta Catenin,
http://linkedlifedata.com/resource/pubmed/chemical/glycogen synthase kinase 3 beta
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AlonNippaN,
pubmed-author:BexFrederick JFJ,
pubmed-author:BhatBheem MBM,
pubmed-author:BursavichMatthew GMG,
pubmed-author:CainMichaelM,
pubmed-author:ColeburnValerieV,
pubmed-author:GilbertAdam MAM,
pubmed-author:GirondaVirginiaV,
pubmed-author:GreenPaulaP,
pubmed-author:HauzeDiane BDB,
pubmed-author:KharodeYogendraY,
pubmed-author:KirisitsMatthewM,
pubmed-author:KrishnamurthyGirijaG,
pubmed-author:LamHo-SunHS,
pubmed-author:LiuYao-BinYB,
pubmed-author:LombardiSabrinaS,
pubmed-author:MatteoJeanneJ,
pubmed-author:MurrillsRichardR,
pubmed-author:RobinsonJohn AJA,
pubmed-author:SelimSallyS,
pubmed-author:SharpMichaelM,
pubmed-author:UnwallaRaymondR,
pubmed-author:VaradarajanUshaU,
pubmed-author:YaworskyPaul JPJ,
pubmed-author:ZhaoWeiguangW
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pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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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 |
366-70
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:19897365-Animals,
pubmed-meshheading:19897365-Bone Development,
pubmed-meshheading:19897365-Cell Line, Tumor,
pubmed-meshheading:19897365-Glycogen Synthase Kinase 3,
pubmed-meshheading:19897365-Humans,
pubmed-meshheading:19897365-Imidazoles,
pubmed-meshheading:19897365-Intercellular Signaling Peptides and Proteins,
pubmed-meshheading:19897365-Mice,
pubmed-meshheading:19897365-Mice, Inbred C57BL,
pubmed-meshheading:19897365-Pyrimidines,
pubmed-meshheading:19897365-Recombinant Fusion Proteins,
pubmed-meshheading:19897365-Signal Transduction,
pubmed-meshheading:19897365-Skull,
pubmed-meshheading:19897365-Wnt Proteins,
pubmed-meshheading:19897365-Wnt3 Protein,
pubmed-meshheading:19897365-Wnt3A Protein,
pubmed-meshheading:19897365-beta Catenin
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pubmed:year |
2010
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pubmed:articleTitle |
Hit to lead studies on (hetero)arylpyrimidines--agonists of the canonical Wnt-beta-catenin cellular messaging system.
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pubmed:affiliation |
Chemical Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, United States. gilbera@wyeth.com
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pubmed:publicationType |
Journal Article
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