1pk5
From Proteopedia
| Line 1: | Line 1: | ||
[[Image:1pk5.gif|left|200px]] | [[Image:1pk5.gif|left|200px]] | ||
| - | + | <!-- | |
| - | + | The line below this paragraph, containing "STRUCTURE_1pk5", creates the "Structure Box" on the page. | |
| - | + | You may change the PDB parameter (which sets the PDB file loaded into the applet) | |
| - | + | or the SCENE parameter (which sets the initial scene displayed when the page is loaded), | |
| - | + | or leave the SCENE parameter empty for the default display. | |
| - | + | --> | |
| - | + | {{STRUCTURE_1pk5| PDB=1pk5 | SCENE= }} | |
| - | + | ||
| - | | | + | |
| - | }} | + | |
'''Crystal structure of the orphan nuclear receptor LRH-1''' | '''Crystal structure of the orphan nuclear receptor LRH-1''' | ||
| Line 29: | Line 26: | ||
[[Category: Krylova, I N.]] | [[Category: Krylova, I N.]] | ||
[[Category: Sablin, E P.]] | [[Category: Sablin, E P.]] | ||
| - | [[Category: | + | [[Category: Ligand-binding domain]] |
| - | [[Category: | + | [[Category: Lrh-1]] |
| - | [[Category: | + | [[Category: Nuclear receptor]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:10:52 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 02:10, 3 May 2008
Crystal structure of the orphan nuclear receptor LRH-1
Overview
The orphan nuclear receptors SF-1 and LRH-1 are constitutively active, but it remains uncertain whether their activation is hormone dependent. We report the crystal structure of the LRH-1 ligand binding domain to 2.4 A resolution and find the receptor to be a monomer that adopts an active conformation with a large but empty hydrophobic pocket. Adding bulky side chains into this pocket resulted in full or greater activity suggesting that, while LRH-1 could accommodate potential ligands, these are dispensable for basal activity. Constitutive LRH-1 activity appears to be conferred by a distinct structural element consisting of an extended helix 2 that provides an additional layer to the canonical LBD fold. Mutating the conserved arginine in helix 2 reduced LRH-1 receptor activity and coregulator recruitment, consistent with the partial loss-of-function phenotype exhibited by an analogous SF-1 human mutant. These findings illustrate an alternative structural strategy for nuclear receptor stabilization in the absence of ligand binding.
About this Structure
1PK5 is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.
Reference
Structural basis for ligand-independent activation of the orphan nuclear receptor LRH-1., Sablin EP, Krylova IN, Fletterick RJ, Ingraham HA, Mol Cell. 2003 Jun;11(6):1575-85. PMID:12820970 Page seeded by OCA on Sat May 3 05:10:52 2008
