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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2009-4-16
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pubmed:abstractText |
The naturally occurring pyranonaphthoquinone (PNQ) antibiotic lactoquinomycin and related aglycones were found to be selective inhibitors of the serine-threonine kinase AKT. A set of synthetic PNQs were prepared and a minimum active feature set and preliminary SAR were determined. PNQ lactones inhibit the proliferation of human tumor cell lines containing constitutively activated AKT and show expected effects on cellular biomarkers. Biochemical data are presented supporting a proposed bioreductive alkylation mechanism of action.
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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 |
Apr
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:DingWei-DongWD,
pubmed-author:EidClarkC,
pubmed-author:HannaCilienC,
pubmed-author:HonoresErickE,
pubmed-author:InsafShabana SSS,
pubmed-author:JohnsonBernardB,
pubmed-author:KrishnamurthyGirijaG,
pubmed-author:LaaksoLeifL,
pubmed-author:LevinJeremy IJI,
pubmed-author:MansourTarek STS,
pubmed-author:MayAA,
pubmed-author:McDonaldLeonard ALA,
pubmed-author:PowellDennisD,
pubmed-author:SalaskiEdward JEJ,
pubmed-author:ShimJaechulJ,
pubmed-author:TabeiKeikoK,
pubmed-author:Toral-BarzaLourdesL,
pubmed-author:YamashitaAyakoA,
pubmed-author:ZhangWei-GuoWG,
pubmed-author:ZhongLiL
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pubmed:issnType |
Electronic
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pubmed:day |
23
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2181-4
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:19309081-Alkylation,
pubmed-meshheading:19309081-Antineoplastic Agents,
pubmed-meshheading:19309081-Biological Markers,
pubmed-meshheading:19309081-Cell Line, Tumor,
pubmed-meshheading:19309081-Cell Proliferation,
pubmed-meshheading:19309081-Cysteine,
pubmed-meshheading:19309081-Humans,
pubmed-meshheading:19309081-Lactones,
pubmed-meshheading:19309081-Naphthoquinones,
pubmed-meshheading:19309081-Oncogene Protein v-akt,
pubmed-meshheading:19309081-Pyrans,
pubmed-meshheading:19309081-Stereoisomerism,
pubmed-meshheading:19309081-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
Pyranonaphthoquinone lactones: a new class of AKT selective kinase inhibitors alkylate a regulatory loop cysteine.
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pubmed:affiliation |
Departments of Chemical & Screening Sciences and Oncology, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA. salaske@wyeth.com
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pubmed:publicationType |
Journal Article
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