3E7C

Glucocorticoid Receptor LBD bound to GSK866

3E7C の概要

• エントリーDOI: 10.2210/pdb3e7c/pdb
• 関連するPDBエントリー: 1m2z
• 分子名称: Glucocorticoid receptor, Nuclear receptor coactivator 2, 5-amino-N-[(2S)-2-({[(2,6-dichlorophenyl)carbonyl](ethyl)amino}methyl)-3,3,3-trifluoro-2-hydroxypropyl]-1-(4-fluorophenyl)-1H-pyrazole-4-carboxamide, ... (5 entities in total)
• 機能のキーワード: gr, glucocorticoid receptor, nuclear receptor, alternative initiation, chromatin regulator, disease mutation, dna-binding, lipid-binding, metal-binding, nucleus, phosphoprotein, pseudohermaphroditism, receptor, steroid-binding, transcription, transcription regulation, zinc-finger, activator
• 由来する生物種: Homo sapiens (Human); 詳細
• 細胞内の位置: Isoform Alpha: Cytoplasm . Isoform Beta: Nucleus . Isoform Alpha-B: Nucleus : P04150; Nucleus: Q15596
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 63783.55

構造登録者

Madauss, K.P.,Williams, S.P.,Mclay, I.,Stewart, E.L.,Bledsoe, R.K. (登録日: 2008-08-18, 公開日: 2008-11-25, 最終更新日: 2024-04-03)

主引用文献

Madauss, K.P.,Bledsoe, R.K.,Mclay, I.,Stewart, E.L.,Uings, I.J.,Weingarten, G.,Williams, S.P.
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.
Bioorg.Med.Chem.Lett., 18:6097-6099, 2008

PubMed Abstract: The amino-pyrazole 2,6-dichloro-N-ethyl benzamide 1 is a selective GR agonist with dexamethasone-like in vitro potency. Its X-ray crystal structure in the GR LBD (Glucocorticoid ligand-binding domain) is described and compared to other reported structures of steroidal GR agonists in the GR LBD (3E7C).

PubMed: 18952422
DOI: 10.1016/j.bmcl.2008.10.021

実験手法

X-RAY DIFFRACTION (2.15 Å)