1n83
From Proteopedia
(New page: 200px<br /> <applet load="1n83" size="450" color="white" frame="true" align="right" spinBox="true" caption="1n83, resolution 1.63Å" /> '''Crystal Structure o...) |
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| - | [[Image:1n83.gif|left|200px]]<br /> | + | [[Image:1n83.gif|left|200px]]<br /><applet load="1n83" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1n83, resolution 1.63Å" /> | caption="1n83, resolution 1.63Å" /> | ||
'''Crystal Structure of the complex between the Orphan Nuclear Hormone Receptor ROR(alpha)-LBD and Cholesterol'''<br /> | '''Crystal Structure of the complex between the Orphan Nuclear Hormone Receptor ROR(alpha)-LBD and Cholesterol'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The retinoic acid-related orphan receptor alpha (RORalpha) is an orphan | + | The retinoic acid-related orphan receptor alpha (RORalpha) is an orphan member of the subfamily 1 of nuclear hormone receptors. No X-ray structure of RORalpha has been described so far, and no ligand has been identified. We describe the first crystal structure of the ligand binding domain (LBD) of RORalpha, at 1.63 A resolution. This structure revealed a ligand present in the ligand binding pocket (LBP), which was identified by X-ray crystallography as cholest-5-en-3beta-ol (cholesterol). Moreover, RORalpha transcriptional activity could be modulated by changes in intracellular cholesterol level or mutation of residues involved in cholesterol binding. These findings suggest that RORalpha could play a key role in the regulation of cholesterol homeostasis and thus represents an important drug target in cholesterol-related diseases. |
==About this Structure== | ==About this Structure== | ||
| - | 1N83 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with CLR as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1N83 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=CLR:'>CLR</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1N83 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Geiser, M.]] | [[Category: Geiser, M.]] | ||
[[Category: Geisse, S.]] | [[Category: Geisse, S.]] | ||
| - | [[Category: Kallen, J | + | [[Category: Kallen, J A.]] |
| - | [[Category: Schlaeppi, J | + | [[Category: Schlaeppi, J M.]] |
[[Category: CLR]] | [[Category: CLR]] | ||
[[Category: dna binding]] | [[Category: dna binding]] | ||
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[[Category: transcription regulation]] | [[Category: transcription regulation]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:03:22 2008'' |
Revision as of 12:03, 21 February 2008
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Crystal Structure of the complex between the Orphan Nuclear Hormone Receptor ROR(alpha)-LBD and Cholesterol
Overview
The retinoic acid-related orphan receptor alpha (RORalpha) is an orphan member of the subfamily 1 of nuclear hormone receptors. No X-ray structure of RORalpha has been described so far, and no ligand has been identified. We describe the first crystal structure of the ligand binding domain (LBD) of RORalpha, at 1.63 A resolution. This structure revealed a ligand present in the ligand binding pocket (LBP), which was identified by X-ray crystallography as cholest-5-en-3beta-ol (cholesterol). Moreover, RORalpha transcriptional activity could be modulated by changes in intracellular cholesterol level or mutation of residues involved in cholesterol binding. These findings suggest that RORalpha could play a key role in the regulation of cholesterol homeostasis and thus represents an important drug target in cholesterol-related diseases.
About this Structure
1N83 is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
Reference
X-ray structure of the hRORalpha LBD at 1.63 A: structural and functional data that cholesterol or a cholesterol derivative is the natural ligand of RORalpha., Kallen JA, Schlaeppi JM, Bitsch F, Geisse S, Geiser M, Delhon I, Fournier B, Structure. 2002 Dec;10(12):1697-707. PMID:12467577
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