6LIT

Estrogen-related receptor beta(ERR2) in complex with BPA

6LIT の概要

• エントリーDOI: 10.2210/pdb6lit/pdb
• 分子名称: Steroid hormone receptor ERR2, 10-mer from Nuclear receptor coactivator 2, 4,4'-PROPANE-2,2-DIYLDIPHENOL, ... (4 entities in total)
• 機能のキーワード: err2, transcription factor, bpa, transcription
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 55775.61

構造登録者

Yao, B.Q.,Li, Y. (登録日: 2019-12-13, 公開日: 2020-10-07, 最終更新日: 2023-11-22)

主引用文献

Yao, B.,Zhang, S.,Wei, Y.,Tian, S.,Lu, Z.,Jin, L.,He, Y.,Xie, W.,Li, Y.
Structural Insights into the Specificity of Ligand Binding and Coactivator Assembly by Estrogen-Related Receptor beta.
J.Mol.Biol., 432:5460-5472, 2020

PubMed Abstract: Estrogen-related receptor β (ERRβ) is a nuclear receptor critical for many biological processes. Despite the biological and pharmaceutical importance of ERRβ, deciphering the structure of ERRβ has been hampered by the difficulties in obtaining a pure and stable protein for structural studies. In fact, the ERRβ ligand-binding domain remains the last unsolved ERR structure and also one of only a few unknown nuclear receptor structures. Here, we report the identification of a critical single-residue mutation resulted in robust solubility and stability of an active ERRβ ligand-binding domain, thereby providing a protein tool enabling the first probe into the biochemical and structural studies of this important receptor. The crystal structure reveals key structural features that have enabled the integration of the molecular determinants of signals transduced across the ligand binding and coregulator recruitment by all three ERR subtypes, which also provides a framework for the rational design of selective and potent ligands for the treatment of various ERR-mediated diseases.

PubMed: 32795533
DOI: 10.1016/j.jmb.2020.08.007

実験手法

X-RAY DIFFRACTION (2 Å)