1h9u

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[[Image:1h9u.jpg|left|200px]]
[[Image:1h9u.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1h9u |SIZE=350|CAPTION= <scene name='initialview01'>1h9u</scene>, resolution 2.70&Aring;
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The line below this paragraph, containing "STRUCTURE_1h9u", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=LGA:Ni+Binding+Site+For+Chain+D'>LGA</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=LG2:6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)CYCLOPROPYL]PYRIDINE-3-CARBOXYLIC+ACID'>LG2</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1h9u| PDB=1h9u | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1h9u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1h9u OCA], [http://www.ebi.ac.uk/pdbsum/1h9u PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1h9u RCSB]</span>
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}}
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'''THE STRUCTURE OF THE HUMAN RETINOID-X-RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH THE SPECIFIC SYNTHETIC AGONIST LG100268'''
'''THE STRUCTURE OF THE HUMAN RETINOID-X-RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH THE SPECIFIC SYNTHETIC AGONIST LG100268'''
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[[Category: Love, J D.]]
[[Category: Love, J D.]]
[[Category: Schwabe, J W.R.]]
[[Category: Schwabe, J W.R.]]
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[[Category: nuclear receptor]]
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[[Category: Nuclear receptor]]
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[[Category: rxr]]
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[[Category: Rxr]]
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[[Category: transcription factor]]
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[[Category: Transcription factor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 18:37:03 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 21:00:46 2008''
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Revision as of 15:37, 2 May 2008

Image:1h9u.jpg

Template:STRUCTURE 1h9u

THE STRUCTURE OF THE HUMAN RETINOID-X-RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH THE SPECIFIC SYNTHETIC AGONIST LG100268


Overview

Ligands that specifically target retinoid-X receptors (RXRs) are emerging as potentially powerful therapies for cancer, diabetes, and the lowering of circulatory cholesterol. To date, RXR has only been crystallized in the absence of ligand or with the promiscuous ligand 9-cis retinoic acid, which also activates retinoic acid receptors. Here we present the structure of hRXRbeta in complex with the RXR-specific agonist LG100268 (LG268). The structure clearly reveals why LG268 is specific for the RXR ligand binding pocket and will not activate retinoic acid receptors. Intriguingly, in the crystals, the C-terminal "activation" helix (AF-2/helix H12) is trapped in a novel position not seen in other nuclear receptor structures such that it does not cap the ligand binding cavity. Mammalian two-hybrid assays indicate that LG268 is unable to release co-repressors from RXR unless co-activators are also present. Together these findings suggest that RXR ligands may be inefficient at repositioning helix H12.

About this Structure

1H9U is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The structural basis for the specificity of retinoid-X receptor-selective agonists: new insights into the role of helix H12., Love JD, Gooch JT, Benko S, Li C, Nagy L, Chatterjee VK, Evans RM, Schwabe JW, J Biol Chem. 2002 Mar 29;277(13):11385-91. Epub 2002 Jan 8. PMID:11782480 Page seeded by OCA on Fri May 2 18:37:03 2008

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