1xiu

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{{STRUCTURE_1xiu| PDB=1xiu | SCENE= }}
{{STRUCTURE_1xiu| PDB=1xiu | SCENE= }}
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'''Crystal structure of the agonist-bound ligand-binding domain of Biomphalaria glabrata RXR'''
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===Crystal structure of the agonist-bound ligand-binding domain of Biomphalaria glabrata RXR===
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==Overview==
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Nuclear receptors form an important class of transcription regulators in metazoans. To learn more about the evolution of these proteins, we have initiated structural studies on nuclear receptor ligand-binding domains from various animals. Here we present the crystal structure of the ligand-binding domain (LBD) of the retinoid X receptor (RXR) from the mollusc Biomphalaria glabrata. The structure reveals a novel tetrameric association in which each monomer is complexed to the human RXR ligand 9-cis retinoic acid and to a human co-activator-derived peptide. The ligand and the co-activator peptide are bound in essentially the same manner as observed in previously reported human RXR LBD structures, suggesting that the mechanisms of RXR-mediated transcription regulation are very similar in mollusc and human. The structure shows further that binding of ligand and co-activator peptide does not necessarily lead to the typical holo-conformation in which helix 12 (H12) folds back and packs against the LBD. Within a canonical dimer, only one monomer is in this closed agonist conformation. The other monomer is in an open conformation with H12 protruding from the LBD core, occupying the H12 interaction groove of another open monomer in an adjacent dimer in a domain swapping fashion, thus resulting in a tetrameric association. Additional tetramer interfaces are formed between H11 of the closed LBD and H6 of the open LBD. This novel holo-tetramer configuration may have a biological role in activating genes whose promoters are poorly recognised by dimers but much more efficiently by the corresponding tetramers.
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{{ABSTRACT_PUBMED_16274693}}
==About this Structure==
==About this Structure==
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[[Category: Protein-ligand complex]]
[[Category: Protein-ligand complex]]
[[Category: Retinoid receptor]]
[[Category: Retinoid receptor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:54:14 2008''

Revision as of 12:54, 28 July 2008

Template:STRUCTURE 1xiu

Crystal structure of the agonist-bound ligand-binding domain of Biomphalaria glabrata RXR

Template:ABSTRACT PUBMED 16274693

About this Structure

1XIU is a Protein complex structure of sequences from Biomphalaria glabrata. Full crystallographic information is available from OCA.

Reference

Crystal structure of a novel tetrameric complex of agonist-bound ligand-binding domain of Biomphalaria glabrata retinoid X receptor., de Groot A, de Rosny E, Juillan-Binard C, Ferrer JL, Laudet V, Pierce RJ, Pebay-Peyroula E, Fontecilla-Camps JC, Borel F, J Mol Biol. 2005 Dec 9;354(4):841-53. Epub 2005 Oct 21. PMID:16274693

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