1y9r
From Proteopedia
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|ACTIVITY= | |ACTIVITY= | ||
|GENE= NR3C2, MCR, MLR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= NR3C2, MCR, MLR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1y9r FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1y9r OCA], [http://www.ebi.ac.uk/pdbsum/1y9r PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1y9r RCSB]</span> | ||
}} | }} | ||
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==Overview== | ==Overview== | ||
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. | 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. | ||
| - | |||
| - | ==Disease== | ||
| - | Known diseases associated with this structure: Hypertension, early-onset, autosomal dominant, with exacerbation in pregnancy OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=600983 600983]], Pseudohypoaldosteronism type I, autosomal dominant OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=600983 600983]] | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Rafestin-Oblin, M E.]] | [[Category: Rafestin-Oblin, M E.]] | ||
[[Category: Rochel, M.]] | [[Category: Rochel, M.]] | ||
| - | [[Category: | + | [[Category: activating mutation]] |
| - | [[Category: mineralocorticoid receptor | + | [[Category: hypertension]] |
| + | [[Category: mineralocorticoid receptor]] | ||
| + | [[Category: nuclear recept]] | ||
| + | [[Category: steroid receptor]] | ||
| + | [[Category: transcription regulation]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:00:37 2008'' |
Revision as of 22:00, 30 March 2008
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| , resolution 1.96Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | NR3C2, MCR, MLR (Homo sapiens) | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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
Overview
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.
About this Structure
1Y9R is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Crystal structure of a mutant mineralocorticoid receptor responsible for hypertension., Fagart J, Huyet J, Pinon GM, Rochel M, Mayer C, Rafestin-Oblin ME, Nat Struct Mol Biol. 2005 Jun;12(6):554-5. Epub 2005 May 22. PMID:15908963
Page seeded by OCA on Mon Mar 31 01:00:37 2008
