2ACL

Liver X-Receptor alpha Ligand Binding Domain with SB313987

2ACL の概要

• エントリーDOI: 10.2210/pdb2acl/pdb
• 分子名称: Retinoic acid receptor RXR-alpha, Oxysterols receptor LXR-alpha, RETINOIC ACID, ... (5 entities in total)
• 機能のキーワード: nuclear hormone receptor ligand binding domain transcription factor three layered a-helix fold, transcription
• 由来する生物種: Homo sapiens (human); 詳細
• 細胞内の位置: Nucleus : P19793 Q9Z0Y9
• タンパク質・核酸の鎖数: 8
• 化学式量合計: 222167.87

構造登録者

Jaye, M.C.,Krawiec, J.A.,Campobasso, N.,Smallwood, A.,Qiu, C.,Lu, Q.,Kerrigan, J.J. (登録日: 2005-07-19, 公開日: 2005-09-20, 最終更新日: 2024-02-14)

主引用文献

Jaye, M.C.,Krawiec, J.A.,Campobasso, N.,Smallwood, A.,Qiu, C.,Lu, Q.,Kerrigan, J.J.,De Los Frailes Alvaro, M.,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.
Discovery of substituted maleimides as liver x receptor agonists and determination of a ligand-bound crystal structure.
J.Med.Chem., 48:5419-5422, 2005

PubMed 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.

PubMed: 16107141
DOI: 10.1021/jm050532w

実験手法

X-RAY DIFFRACTION (2.8 Å)