1k4w

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{{STRUCTURE_1k4w| PDB=1k4w | SCENE= }}
{{STRUCTURE_1k4w| PDB=1k4w | SCENE= }}
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'''X-ray structure of the orphan nuclear receptor ROR beta ligand-binding domain in the active conformation'''
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===X-ray structure of the orphan nuclear receptor ROR beta ligand-binding domain in the active conformation===
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==Overview==
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The retinoic acid-related orphan receptor beta (RORbeta) exhibits a highly restricted neuronal-specific expression pattern in brain, retina and pineal gland. So far, neither a natural RORbeta target gene nor a functional ligand have been identified, and the physiological role of the receptor is not well understood. We present the crystal structure of the ligand-binding domain (LBD) of RORbeta containing a bound stearate ligand and complexed with a coactivator peptide. In the crystal, the monomeric LBD adopts the canonical agonist-bound form. The fatty acid ligand-coactivator peptide combined action stabilizes the transcriptionally active conformation. The large ligand-binding pocket is strictly hydrophobic on the AF-2 side and more polar on the beta-sheet side where the carboxylate group of the ligand binds. Site-directed mutagenesis experiments validate the significance of the present structure. Homology modeling of the other isotypes will help to design isotype-selective agonists and antagonists that can be used to characterize the physiological functions of RORs. In addition, our crystallization strategy can be extended to other orphan nuclear receptors, providing a powerful tool to delineate their functions.
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(as it appears on PubMed at http://www.pubmed.gov), where 11689423 is the PubMed ID number.
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{{ABSTRACT_PUBMED_11689423}}
==About this Structure==
==About this Structure==
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[[Category: Ligand-binding domain]]
[[Category: Ligand-binding domain]]
[[Category: Transcriptionally active conformation]]
[[Category: Transcriptionally active conformation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 22:18:43 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 09:47:06 2008''

Revision as of 06:47, 2 July 2008

Image:1k4w.png

Template:STRUCTURE 1k4w

X-ray structure of the orphan nuclear receptor ROR beta ligand-binding domain in the active conformation

Template:ABSTRACT PUBMED 11689423

About this Structure

1K4W is a Protein complex structure of sequences from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

X-ray structure of the orphan nuclear receptor RORbeta ligand-binding domain in the active conformation., Stehlin C, Wurtz JM, Steinmetz A, Greiner E, Schule R, Moras D, Renaud JP, EMBO J. 2001 Nov 1;20(21):5822-31. PMID:11689423

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