1n4h

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{{STRUCTURE_1n4h| PDB=1n4h | SCENE= }}
{{STRUCTURE_1n4h| PDB=1n4h | SCENE= }}
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'''Characterization of ligands for the orphan nuclear receptor RORbeta'''
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===Characterization of ligands for the orphan nuclear receptor RORbeta===
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==Overview==
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Retinoids regulate gene expression through binding to the nuclear retinoic acid receptors (RARs) and retinoid X receptors (RXRs). In contrast, no ligands for the retinoic acid receptor-related orphan receptors beta and gamma (ROR beta and gamma) have been identified, yet structural data and structure-function analyses indicate that ROR beta is a ligand-regulated nuclear receptor. Using nondenaturing mass spectrometry and scintillation proximity assays we found that all-trans retinoic acid (ATRA) and several retinoids bind to the ROR beta ligand-binding domain (LBD). The crystal structures of the complex with ATRA and with the synthetic analog ALRT 1550 reveal the binding modes of these ligands. ATRA and related retinoids inhibit ROR beta but not ROR alpha transcriptional activity suggesting that high-affinity, subtype-specific ligands could be designed for the identification of ROR beta target genes. Our results identify ROR beta as a retinoid-regulated nuclear receptor, providing a novel pathway for retinoid action.
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(as it appears on PubMed at http://www.pubmed.gov), where 12958591 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12958591}}
==About this Structure==
==About this Structure==
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 02:05:02 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 07:57:14 2008''

Revision as of 04:57, 29 July 2008

Image:1n4h.png

Template:STRUCTURE 1n4h

Characterization of ligands for the orphan nuclear receptor RORbeta

Template:ABSTRACT PUBMED 12958591

About this Structure

1N4H is a Protein complex structure of sequences from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta., Stehlin-Gaon C, Willmann D, Zeyer D, Sanglier S, Van Dorsselaer A, Renaud JP, Moras D, Schule R, Nat Struct Biol. 2003 Oct;10(10):820-5. Epub 2003 Sep 7. PMID:12958591

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