Source:http://linkedlifedata.com/resource/pubmed/id/19427203
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
2009-5-29
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pubmed:abstractText |
The synthesis and biological evaluation of JAK3 based staurosporine compounds is described. The compounds are constructed completely de novo, and a ring closing metathesis strategy is used to assemble the sugar mimetic portion. These analogs show potent JAK3 activity against isolated enzyme and in T-cells. One analog (32) showed unique biological effects during in vitro and in vivo tests including inhibition of STAT5 phosphorylation, blockade of mast cell responses, and reduction of JAK3 based effects in mice models of allergic disease.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3333-8
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:19427203-Animals,
pubmed-meshheading:19427203-Cyclization,
pubmed-meshheading:19427203-Drug Evaluation, Preclinical,
pubmed-meshheading:19427203-Hypersensitivity,
pubmed-meshheading:19427203-Janus Kinase 3,
pubmed-meshheading:19427203-Mast Cells,
pubmed-meshheading:19427203-Mice,
pubmed-meshheading:19427203-Phosphorylation,
pubmed-meshheading:19427203-Protein Kinase Inhibitors,
pubmed-meshheading:19427203-STAT5 Transcription Factor,
pubmed-meshheading:19427203-Staurosporine,
pubmed-meshheading:19427203-Structure-Activity Relationship,
pubmed-meshheading:19427203-T-Lymphocytes
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pubmed:year |
2009
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pubmed:articleTitle |
Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.
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pubmed:affiliation |
High Throughput Chemistry Department, Johnson & Johnson Pharmaceutical Research & Development L.L.C. 920 Route 202, PO Box 300, Raritan, NJ 08869, USA. wilsonlarr@gmail.com
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pubmed:publicationType |
Journal Article
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