Discovery of Substituted Maleimides as Liver X Receptor Agonists and Determination of a Ligand-Bound Crystal Structure
Year: 2005
Type: article
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.
Source: Journal of Medicinal Chemistry
DOI: 10.1021/jm050532w
Authors: Michael C. Jaye, 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
Institution: GlaxoSmithKline (United States)
Language: English
Subfield: Surgery
Field: Medicine
Domain: Health Sciences
Open Access status: green
OpenAlex ID: W2085710563