2ZBS

Crystal structure of human estrogen-related receptor gamma ligand binding domain apo form

2ZBS の概要

• エントリーDOI: 10.2210/pdb2zbs/pdb
• 関連するPDBエントリー: 2E2R 2ZAS
• 分子名称: Estrogen-related receptor gamma (2 entities in total)
• 機能のキーワード: err gamma, nuclear receptor, transcription, apo form, activator, alternative splicing, dna-binding, metal-binding, nucleus, polymorphism, transcription regulation, zinc, zinc-finger
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Nucleus (Probable): P62508
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 27611.14

構造登録者

Matsushima, A.,Kakuta, Y.,Teramoto, T.,Shimohigashi, Y. (登録日: 2007-10-27, 公開日: 2008-10-07, 最終更新日: 2023-11-01)

主引用文献

Matsushima, A.,Teramoto, T.,Okada, H.,Liu, X.,Tokunaga, T.,Kakuta, Y.,Shimohigashi, Y.
ERRgamma tethers strongly bisphenol A and 4-alpha-cumylphenol in an induced-fit manner
Biochem.Biophys.Res.Commun., 373:408-413, 2008

PubMed Abstract: A receptor-binding assay and X-ray crystal structure analysis demonstrated that the endocrine disruptor bisphenol A (BPA) strongly binds to human estrogen-related receptor gamma (ERRgamma). BPA is well anchored to the ligand-binding pocket, forming hydrogen bonds with its two phenol-hydroxyl groups. In this study, we found that 4-alpha-cumylphenol lacking one of its phenol-hydroxyl groups also binds to ERRgamma very strongly. The 2.0 A crystal structure of the 4-alpha-cumylphenol/ERRgamma complex clearly revealed that ERRgamma's Leu345-beta-isopropyl plays a role in the tight binding of 4-alpha-cumylphenol and BPA, rotating in a back-and-forth induced-fit manner.

PubMed: 18582436
DOI: 10.1016/j.bbrc.2008.06.050

実験手法

X-RAY DIFFRACTION (1.8 Å)