2qe4

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[[Image:2qe4.jpg|left|200px]]
[[Image:2qe4.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2qe4 |SIZE=350|CAPTION= <scene name='initialview01'>2qe4</scene>, resolution 2.40&Aring;
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The line below this paragraph, containing "STRUCTURE_2qe4", creates the "Structure Box" on the page.
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|SITE=
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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=JJ3:(3AS,4R,9BR)-4-(4-HYDROXYPHENYL)-6-(METHOXYMETHYL)-1,2,3,3A,4,9B-HEXAHYDROCYCLOPENTA[C]CHROMEN-8-OL'>JJ3</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= ESR1, ESR, NR3A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2qe4| PDB=2qe4 | SCENE= }}
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|RELATEDENTRY=[[2q70|2Q70]], [[2i0j|2I0J]], [[2pog|2POG]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2qe4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2qe4 OCA], [http://www.ebi.ac.uk/pdbsum/2qe4 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2qe4 RCSB]</span>
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}}
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'''Estrogen receptor alpha ligand-binding domain in complex with a benzopyran agonist'''
'''Estrogen receptor alpha ligand-binding domain in complex with a benzopyran agonist'''
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[[Category: Ryter, K T.]]
[[Category: Ryter, K T.]]
[[Category: Wang, Y.]]
[[Category: Wang, Y.]]
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[[Category: alternative splicing]]
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[[Category: Alternative splicing]]
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[[Category: dna-binding]]
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[[Category: Dna-binding]]
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[[Category: ligand-binding domain]]
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[[Category: Ligand-binding domain]]
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[[Category: lipid-binding]]
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[[Category: Lipid-binding]]
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[[Category: metal-binding]]
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[[Category: Metal-binding]]
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[[Category: nuclear protein]]
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[[Category: Nuclear protein]]
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[[Category: nuclear receptor]]
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[[Category: Nuclear receptor]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: polymorphism]]
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[[Category: Polymorphism]]
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[[Category: steroid-binding]]
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[[Category: Steroid-binding]]
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[[Category: transcription]]
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[[Category: Transcription]]
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[[Category: transcription regulation]]
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[[Category: Transcription regulation]]
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[[Category: zinc]]
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[[Category: Zinc]]
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[[Category: zinc-finger]]
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[[Category: Zinc-finger]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:47:50 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:48:11 2008''
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Revision as of 11:47, 4 May 2008

Image:2qe4.jpg

Template:STRUCTURE 2qe4

Estrogen receptor alpha ligand-binding domain in complex with a benzopyran agonist


Overview

Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER receptor subtypes alpha and beta in opposite orientations. We have used structure based drug design to show that this unique phenomena can be exploited via substitution at the 8-position of the benzopyran A-ring to disrupt binding to ERalpha, thus improving ERbeta subtype selectivity. X-ray cocrystal structures with ERalpha and ERbeta are supportive of this approach to improve selectivity in this structural class.

About this Structure

2QE4 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 4: functionalization of the benzopyran A-ring., Norman BH, Richardson TI, Dodge JA, Pfeifer LA, Durst GL, Wang Y, Durbin JD, Krishnan V, Dinn SR, Liu S, Reilly JE, Ryter KT, Bioorg Med Chem Lett. 2007 Sep 15;17(18):5082-5. Epub 2007 Jul 13. PMID:17662603 Page seeded by OCA on Sun May 4 14:47:50 2008

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OCA

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