1YA3

Crystal structure of the human mineralocorticoid receptor ligand-binding domain bound to progesterone and harboring the S810L mutation responsible for a severe form of hypertension

1YA3 の概要

• エントリーDOI: 10.2210/pdb1ya3/pdb
• 分子名称: Mineralocorticoid receptor, PROGESTERONE (3 entities in total)
• 機能のキーワード: mineralocorticoid receptor, steroid receptor, nuclear receptor transcription regulation, activating mutation, hypertension, transcription
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm: P08235
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 89876.46

構造登録者

Fagart, J.,Huyet, J.,Pinon, G.M.,Rochel, M.,Mayer, C.,Rafestin-Oblin, M.E. (登録日: 2004-12-17, 公開日: 2005-05-24, 最終更新日: 2023-08-23)

主引用文献

Fagart, J.,Huyet, J.,Pinon, G.M.,Rochel, M.,Mayer, C.,Rafestin-Oblin, M.E.
Crystal structure of a mutant mineralocorticoid receptor responsible for hypertension
Nat.Struct.Mol.Biol., 12:554-555, 2005

PubMed Abstract: The S810L mutation within the human mineralocorticoid receptor (MR S810L) induces severe hypertension and switches progesterone from antagonist to agonist. Here we report the crystal structures of the ligand-binding domain of MR S810L in complex with progesterone and deoxycorticosterone, an agonist of both wild-type and mutant MRs. These structures, the first for MR, identify the specific contacts created by Leu810 and clarify the mechanism of activation of MR S810L.

PubMed: 15908963
DOI: 10.1038/nsmb939

実験手法

X-RAY DIFFRACTION (2.34 Å)