| Literature DB >> 16107141 |
Michael C Jaye1, John A Krawiec, Nino Campobasso, Angela Smallwood, Chunyan Qiu, Quinn Lu, John J Kerrigan, Maite De Los Frailes Alvaro, Bryan Laffitte, Wu-Schyong Liu, Joseph P Marino, Craig R Meyer, Jason A Nichols, Derek J Parks, Paloma Perez, Lea Sarov-Blat, Sheila D Seepersaud, Klaudia M Steplewski, Scott K Thompson, Ping Wang, Mike A Watson, Christine L Webb, David Haigh, Justin A Caravella, Colin H Macphee, Timothy M Willson, Jon L Collins.
Abstract
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 as an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta 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.Entities:
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Year: 2005 PMID： 16107141 DOI： 10.1021/jm050532w
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446