Source:http://linkedlifedata.com/resource/pubmed/id/21185721
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2
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| pubmed:dateCreated |
2011-1-11
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| pubmed:abstractText |
S6K1 (p70 S6 kinase-1) is thought to play a critical role in the development of obesity and insulin resistance, thus making it an attractive target in developing medicines for the treatment of these disorders. We describe a novel thiophene urea class of S6K inhibitors. The lead matter for the development of these inhibitors came from mining the literature for reports of weak off-target S6K activity. These optimized inhibitors exhibit good potency and excellent selectivity for S6K over a panel of 43 kinases.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical | |
| pubmed:status |
MEDLINE
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| pubmed:month |
Jan
|
| pubmed:issn |
1464-3405
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| pubmed:author | |
| pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
|
| pubmed:issnType |
Electronic
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| pubmed:day |
15
|
| pubmed:volume |
21
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
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| pubmed:pagination |
849-52
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| pubmed:meshHeading |
pubmed-meshheading:21185721-Humans,
pubmed-meshheading:21185721-Microsomes, Liver,
pubmed-meshheading:21185721-Protein Kinase Inhibitors,
pubmed-meshheading:21185721-Ribosomal Protein S6 Kinases, 70-kDa,
pubmed-meshheading:21185721-Structure-Activity Relationship,
pubmed-meshheading:21185721-Thiophenes,
pubmed-meshheading:21185721-Urea
|
| pubmed:year |
2011
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| pubmed:articleTitle |
Potent and selective thiophene urea-templated inhibitors of S6K.
|
| pubmed:affiliation |
Cambridge South Laboratory, Pfizer Inc., 620 Memorial Drive, Cambridge, MA 02139, United States.
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| pubmed:publicationType |
Journal Article
|