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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 |
2010-9-20
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pubmed:abstractText |
Starting from HTS hit 1a, X-ray co-crystallization and molecular modeling were used to design potent and selective inhibitors of PI3-kinase. Bioavailablity in this series was improved through careful modulation of physicochemical properties. Compound 12 displayed in vivo knockdown of PI3K pharmacodynamic markers such as pAKT, pPRAS40, and pS6RP in a PC3 prostate cancer xenograft 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 |
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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:BhatSeema RSR,
pubmed-author:CastanedoGeorgette MGM,
pubmed-author:ChuckowreeIrina SIS,
pubmed-author:DotsonJennaJ,
pubmed-author:FolkesAdrian JAJ,
pubmed-author:FriedmanLori SLS,
pubmed-author:HeffronTimothy PTP,
pubmed-author:LeeLeslieL,
pubmed-author:LesnickJohnJ,
pubmed-author:LewisCristinaC,
pubmed-author:MurrayJeremy MJM,
pubmed-author:NonomiyaJimJ,
pubmed-author:OliveroAlan GAG,
pubmed-author:PangJodieJ,
pubmed-author:PliseEmileE,
pubmed-author:PriorWei WeiWW,
pubmed-author:RougeLionelL,
pubmed-author:SalphatiLaurentL,
pubmed-author:SampathDeepakD,
pubmed-author:StabenSteven TST,
pubmed-author:SutherlinDaniel PDP,
pubmed-author:TsuiVickieV,
pubmed-author:WanNan ChiNC,
pubmed-author:WangShumeiS,
pubmed-author:WeismannChristianC,
pubmed-author:WuPingP,
pubmed-author:ZhuBing-YanBY
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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 |
6048-51
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pubmed:meshHeading |
pubmed-meshheading:20822905-Animals,
pubmed-meshheading:20822905-Cell Line,
pubmed-meshheading:20822905-Crystallography, X-Ray,
pubmed-meshheading:20822905-Humans,
pubmed-meshheading:20822905-Male,
pubmed-meshheading:20822905-Mice,
pubmed-meshheading:20822905-Models, Molecular,
pubmed-meshheading:20822905-Phosphatidylinositol 3-Kinases,
pubmed-meshheading:20822905-Prostatic Neoplasms,
pubmed-meshheading:20822905-Protein Kinase Inhibitors,
pubmed-meshheading:20822905-Pyrazoles,
pubmed-meshheading:20822905-Pyridines,
pubmed-meshheading:20822905-Pyrimidines,
pubmed-meshheading:20822905-Rats,
pubmed-meshheading:20822905-Solubility,
pubmed-meshheading:20822905-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.
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pubmed:affiliation |
Discovery Chemistry, Genentech, Inc., South San Francisco, CA 94080, USA. stevents@gene.com
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pubmed:publicationType |
Journal Article
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