1Y9R

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

Summary for 1Y9R

• Entry DOI: 10.2210/pdb1y9r/pdb
• Descriptor: Mineralocorticoid receptor, DESOXYCORTICOSTERONE (3 entities in total)
• Functional Keywords: mineralocorticoid receptor; steroid receptor; nuclear recept; transcription regulation; activating mutation; hypertension, transcription, ligand binding protein
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm: P08235
• Total number of polymer chains: 2
• Total formula weight: 59949.64

Authors

Fagart, J.,Huyet, J.,Pinon, G.M.,Rochel, M.,Mayer, C.,Rafestin-Oblin, M.E. (deposition date: 2004-12-16, release date: 2005-05-24, Last modification date: 2024-04-03)

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 (1.96 Å)