Source:http://linkedlifedata.com/resource/pubmed/id/16737814
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
15
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| pubmed:dateCreated |
2006-6-20
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| pubmed:abstractText |
In the quest for novel PPARalpha/gamma co-agonists as putative drugs for the treatment of type 2 diabetes and dyslipidemia, we have used a structure-based design approach to identify propionic acids with a 1,5-disubstituted indole scaffold as potent PPARalpha/gamma activators. Compounds 13, 24, and 28 are examples of submicromolar dual agonists with different alpha/gamma EC50 ratios that are selective against the delta-isoform. Analysis of the X-ray complex structure of PPARgamma with the indole propionic acid 13 provides a rationalization for some of the observed SAR.
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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
|
| pubmed:month |
Aug
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| pubmed:issn |
0960-894X
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
1
|
| pubmed:volume |
16
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
4016-20
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| pubmed:meshHeading |
pubmed-meshheading:16737814-Drug Design,
pubmed-meshheading:16737814-Indoles,
pubmed-meshheading:16737814-Molecular Structure,
pubmed-meshheading:16737814-PPAR alpha,
pubmed-meshheading:16737814-PPAR gamma,
pubmed-meshheading:16737814-Structure-Activity Relationship,
pubmed-meshheading:16737814-X-Ray Diffraction
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| pubmed:year |
2006
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| pubmed:articleTitle |
Structure-based design of indole propionic acids as novel PPARalpha/gamma co-agonists.
|
| pubmed:affiliation |
F. Hoffmann-La Roche Ltd, Discovery Research Basel, CH-4070 Basel, Switzerland. bernd.kuhn@roche.com
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| pubmed:publicationType |
Journal Article
|