4OZT

crystal structure of the ligand binding domains of the Bovicola ovis ecdysone receptor EcR/USP heterodimer (PonA crystal)

4OZT の概要

• エントリーDOI: 10.2210/pdb4ozt/pdb
• 関連するPDBエントリー: 4OZR
• 分子名称: Ecdysone receptor, Retinoid X receptor, 2,3,14,20,22-PENTAHYDROXYCHOLEST-7-EN-6-ONE, ... (5 entities in total)
• 機能のキーワード: ecdysone receptor, usp, pona, transcription
• 由来する生物種: Pediculus humanus subsp. corporis (Body louse); 詳細
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 50049.93

構造登録者

Ren, B.,Peat, T.S.,Streltsov, V.A.,Pollard, M.,Fernley, R.,Grusovin, J.,Seabrook, S.,Pilling, P.,Phan, T.,Lu, L.,Lovrecz, G.O.,Graham, L.D.,Hill, R.J. (登録日: 2014-02-19, 公開日: 2014-07-30, 最終更新日: 2023-12-27)

主引用文献

Ren, B.,Peat, T.S.,Streltsov, V.A.,Pollard, M.,Fernley, R.,Grusovin, J.,Seabrook, S.,Pilling, P.,Phan, T.,Lu, L.,Lovrecz, G.O.,Graham, L.D.,Hill, R.J.
Unprecedented conformational flexibility revealed in the ligand-binding domains of the Bovicola ovis ecdysone receptor (EcR) and ultraspiracle (USP) subunits.
Acta Crystallogr.,Sect.D, 70:1954-1964, 2014

PubMed Abstract: The heterodimeric ligand-binding region of the Bovicola ovis ecdysone receptor has been crystallized either in the presence of an ecdysteroid or a synthetic methylene lactam insecticide. Two X-ray crystallographic structures, determined at 2.7 Å resolution, show that the ligand-binding domains of both subunits of this receptor, like those of other nuclear receptors, can display significant conformational flexibility. Thermal melt experiments show that while ponasterone A stabilizes the higher order structure of the heterodimer in solution, the methylene lactam destabilizes it. The conformations of the EcR and USP subunits observed in the structure crystallized in the presence of the methylene lactam have not been seen previously in any ecdysone receptor structure and represent a new level of conformational flexibility for these important receptors. Interestingly, the new USP conformation presents an open, unoccupied ligand-binding pocket.

PubMed: 25004972
DOI: 10.1107/S1399004714009626

実験手法

X-RAY DIFFRACTION (2.7 Å)