Source:http://linkedlifedata.com/resource/pubmed/id/15261265
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
16
|
| pubmed:dateCreated |
2004-7-20
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| pubmed:abstractText |
The synthesis, activity, metabolic stability, and pharmacokinetics of steroidal and nonsteroidal glucocorticoid receptor modulator-statin hybrids is reported. Potent steroidal antagonist-statin hybrids like 22 (h-GR binding IC(50)=7 nM) and nonsteroidal modulator hybrids like 16 (h-GR binding IC(50)=2 nM) were discovered. Appending a 'statin'-like diol-acid group to the modulators dramatically improved metabolic stability (and in some cases hepatocyte activity), but did not impart hepatoselectivity.
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| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Aug
|
| pubmed:issn |
0960-894X
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| pubmed:author |
pubmed-author:CarrollSherryS,
pubmed-author:DengDaisyD,
pubmed-author:EmeryMauriceM,
pubmed-author:FungStevenS,
pubmed-author:Goos-NilssonAnnikaA,
pubmed-author:GrynfarbMarlenaM,
pubmed-author:LaiChunqiuC,
pubmed-author:LindJ MJM,
pubmed-author:SorensenBryan KBK,
pubmed-author:Von GeldernThomasT,
pubmed-author:WangJiahongJ
|
| pubmed:issnType |
Print
|
| pubmed:day |
16
|
| pubmed:volume |
14
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
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| pubmed:pagination |
4173-8
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| pubmed:meshHeading | |
| pubmed:year |
2004
|
| pubmed:articleTitle |
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.
|
| pubmed:affiliation |
Metabolic Disease Research, Abbott Laboratories, Dept 4 CB, Bldg. AP-10, Rm. L-14, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. james.link@abbott.com
|
| pubmed:publicationType |
Journal Article
|