Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure
| Data(s) |
25/08/2005
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| Resumo |
Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a high throughput screen as inducers of human ATP binding cassette transporter A1 expression. Mechanism of action studies led to the identification of GSK3987 (4) as an LXR ligand. 4 recruits the steroid receptor coactivator-1 to human LXR alpha and LXRP with EC(50)s of 40 nM, profiles as an LXR agonist in functional assays, and activates LXR though a mechanism that is similar to first generation LXR agonists. |
| Identificador |
http://dx.doi.org/10.1021/jm050532w http://www.scopus.com/inward/record.url?scp=23944439351&partnerID=8YFLogxK |
| Idioma(s) |
eng |
| Direitos |
info:eu-repo/semantics/restrictedAccess |
| Fonte |
Jaye , M C , Krawiec , J A , Campobasso , N , Smallwood , A , Qiu , C Y , Lu , Q , Kerrigan , J J , Alvaro , M D L , Laffitte , B , Liu , W S , Marino , J P , Meyer , C R , Nichols , J A , Parks , D J , Perez , P , Sarov-Blat , L , Seepersaud , S D , Steplewski , K M , Thompson , S K , Wang , P , Watson , M A , Webb , C L , Haigh , D , Caravella , J A , Macphee , C H , Willson , T M & Collins , J L 2005 , ' Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure ' Journal of Medicinal Chemistry , vol 48 , no. 17 , pp. 5419-5422 . DOI: 10.1021/jm050532w |
| Palavras-Chave | #/dk/atira/pure/subjectarea/asjc/1600/1605 #Organic Chemistry |
| Tipo |
article |
