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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2002-2-21
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pubmed:abstractText |
Screening of our internal compound collection for inhibitors of the transforming growth factor beta1 (TGF-beta1) type I receptor (ALK5) identified several hits. Optimization of the dihydropyrroloimidazole hit 2 by introduction of a 2-pyridine and 3,4-methylenedioxyphenyl group gave 7, a selective ALK5 inhibitor. With this information, optimization of the triarylimidazole hit 8 gave the selective inhibitor 14, which inhibits TGF-beta1-induced fibronectin mRNA formation while displaying no measurable cytotoxicity in the 48 h XTT assay.
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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/Activin Receptors, Type I,
http://linkedlifedata.com/resource/pubmed/chemical/DNA-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Fibronectins,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Mitogen-Activated Protein Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Protein-Serine-Threonine Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/RNA, Messenger,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Transforming Growth...,
http://linkedlifedata.com/resource/pubmed/chemical/SMAD3 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Smad3 Protein,
http://linkedlifedata.com/resource/pubmed/chemical/TGF-beta type I receptor,
http://linkedlifedata.com/resource/pubmed/chemical/Trans-Activators,
http://linkedlifedata.com/resource/pubmed/chemical/p38 Mitogen-Activated Protein...
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BurgessJoelle LJL,
pubmed-author:CallahanJames FJF,
pubmed-author:FornwaldJames AJA,
pubmed-author:GasterLaramie MLM,
pubmed-author:HarlingJohn DJD,
pubmed-author:HarringtonFrank PFP,
pubmed-author:HeerJagJ,
pubmed-author:KwonChetC,
pubmed-author:LapingNicholas JNJ,
pubmed-author:LehrRuthR,
pubmed-author:MathurAA,
pubmed-author:OlsonBarbara ABA,
pubmed-author:WeinstockJosephJ
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pubmed:issnType |
Print
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pubmed:day |
28
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
999-1001
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:11855979-Activin Receptors, Type I,
pubmed-meshheading:11855979-DNA-Binding Proteins,
pubmed-meshheading:11855979-Enzyme Inhibitors,
pubmed-meshheading:11855979-Fibronectins,
pubmed-meshheading:11855979-Humans,
pubmed-meshheading:11855979-Imidazoles,
pubmed-meshheading:11855979-Mitogen-Activated Protein Kinases,
pubmed-meshheading:11855979-Protein-Serine-Threonine Kinases,
pubmed-meshheading:11855979-RNA, Messenger,
pubmed-meshheading:11855979-Receptors, Transforming Growth Factor beta,
pubmed-meshheading:11855979-Smad3 Protein,
pubmed-meshheading:11855979-Structure-Activity Relationship,
pubmed-meshheading:11855979-Trans-Activators,
pubmed-meshheading:11855979-Tumor Cells, Cultured,
pubmed-meshheading:11855979-p38 Mitogen-Activated Protein Kinases
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pubmed:year |
2002
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pubmed:articleTitle |
Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).
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pubmed:affiliation |
Department of Medicinal Chemistry, GlaxoSmithKline Pharmaceuticals, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA. james_f_callahan@gsk.com
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pubmed:publicationType |
Journal Article
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