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

Summary for 1YA3

• Entry DOI: 10.2210/pdb1ya3/pdb
• Descriptor: Mineralocorticoid receptor, PROGESTERONE (3 entities in total)
• Functional Keywords: mineralocorticoid receptor, steroid receptor, nuclear receptor transcription regulation, activating mutation, hypertension, transcription
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm: P08235
• Total number of polymer chains: 3
• Total formula weight: 89876.46

Authors

Fagart, J.,Huyet, J.,Pinon, G.M.,Rochel, M.,Mayer, C.,Rafestin-Oblin, M.E. (deposition date: 2004-12-17, release date: 2005-05-24, Last modification date: 2023-08-23)

Primary citation

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

Experimental method

X-RAY DIFFRACTION (2.34 Å)