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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
15
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pubmed:dateCreated |
2010-7-16
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pubmed:abstractText |
Pyridopyridazine antagonists of the hedgehog signaling pathway are described. Designed to optimize our previously described phthalazine smoothened antagonists, a representative compound eliminates a PXR liability while retaining potency and in vitro metabolic stability. Moreover, the compound has improved efficacy in a hedgehog/smoothened signaling mouse pharmacodynamic model.
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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/4-'demycarosyl-20-deoxo-20-(di-N-ben...,
http://linkedlifedata.com/resource/pubmed/chemical/Hedgehog Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Phthalazines,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridazines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, G-Protein-Coupled,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Steroid,
http://linkedlifedata.com/resource/pubmed/chemical/SMO protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Tylosin,
http://linkedlifedata.com/resource/pubmed/chemical/phthalazine,
http://linkedlifedata.com/resource/pubmed/chemical/pregnane X receptor,
http://linkedlifedata.com/resource/pubmed/chemical/pyridazine
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AaronWadeW,
pubmed-author:AnSongzhuS,
pubmed-author:AustinRichardR,
pubmed-author:BrownMattM,
pubmed-author:ChongAngelaA,
pubmed-author:HOWEE SES,
pubmed-author:HuangTomT,
pubmed-author:HungateRandallR,
pubmed-author:JiangBenB,
pubmed-author:JohnsonMichael GMG,
pubmed-author:KaizermanJacob AJA,
pubmed-author:LucasBrian SBS,
pubmed-author:McMinnDustin LDL,
pubmed-author:OrfJessicaJ,
pubmed-author:RongMinqingM,
pubmed-author:TotevaMaria MMM,
pubmed-author:WickramasingheDineliD,
pubmed-author:XuGuifenG,
pubmed-author:YeQiupingQ,
pubmed-author:ZhongWendyW
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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 |
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 |
4607-10
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pubmed:meshHeading |
pubmed-meshheading:20594845-Animals,
pubmed-meshheading:20594845-Hedgehog Proteins,
pubmed-meshheading:20594845-Humans,
pubmed-meshheading:20594845-Mice,
pubmed-meshheading:20594845-Microsomes, Liver,
pubmed-meshheading:20594845-Phthalazines,
pubmed-meshheading:20594845-Piperazines,
pubmed-meshheading:20594845-Pyridazines,
pubmed-meshheading:20594845-Rats,
pubmed-meshheading:20594845-Receptors, G-Protein-Coupled,
pubmed-meshheading:20594845-Receptors, Steroid,
pubmed-meshheading:20594845-Signal Transduction,
pubmed-meshheading:20594845-Structure-Activity Relationship,
pubmed-meshheading:20594845-Tylosin
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pubmed:year |
2010
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pubmed:articleTitle |
Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.
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pubmed:affiliation |
Amgen, Inc., South San Francisco, CA 94080, USA.
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pubmed:publicationType |
Journal Article
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