1h9u

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[[Image:1h9u.jpg|left|200px]]<br /><applet load="1h9u" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1h9u.jpg|left|200px]]
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caption="1h9u, resolution 2.70&Aring;" />
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'''THE STRUCTURE OF THE HUMAN RETINOID-X-RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH THE SPECIFIC SYNTHETIC AGONIST LG100268'''<br />
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{{Structure
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|PDB= 1h9u |SIZE=350|CAPTION= <scene name='initialview01'>1h9u</scene>, resolution 2.70&Aring;
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|SITE= <scene name='pdbsite=LGA:Ni+Binding+Site+For+Chain+D'>LGA</scene>
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|LIGAND= <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene> and <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>
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|ACTIVITY=
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|GENE=
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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'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1H9U 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=NI:'>NI</scene>, <scene name='pdbligand=CL:'>CL</scene> and <scene name='pdbligand=LG2:'>LG2</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Known structural/functional Site: <scene name='pdbsite=LGA:Ni+Binding+Site+For+Chain+D'>LGA</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1H9U OCA].
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1H9U is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1H9U OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=11782480 11782480]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/11782480 11782480]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: transcription factor]]
[[Category: transcription factor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:58:59 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 11:34:25 2008''

Revision as of 09:34, 20 March 2008

Image:1h9u.jpg


PDB ID 1h9u

Drag the structure with the mouse to rotate
, resolution 2.70Å
Sites:
Ligands: , and
Coordinates: save as pdb, mmCIF, xml



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

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