2ewp

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[[Image:2ewp.gif|left|200px]]
[[Image:2ewp.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2ewp |SIZE=350|CAPTION= <scene name='initialview01'>2ewp</scene>, resolution 2.30&Aring;
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The line below this paragraph, containing "STRUCTURE_2ewp", 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=TXF:(Z)-4-(1-{4-[2-(DIMETHYLAMINO)ETHOXY]PHENYL}-5-HYDROXY-2-PHENYLPENT-1-ENYL)PHENOL'>TXF</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= ESRRG, ERR3, ERRG2, KIAA0832, NR3B3 ([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_2ewp| PDB=2ewp | 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=2ewp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ewp OCA], [http://www.ebi.ac.uk/pdbsum/2ewp PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ewp RCSB]</span>
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}}
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'''Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182'''
'''Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Nolte, R T.]]
[[Category: Nolte, R T.]]
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[[Category: err]]
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[[Category: Err]]
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[[Category: estrogen related receptor]]
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[[Category: Estrogen related receptor]]
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[[Category: orphan receptor]]
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[[Category: Orphan receptor]]
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[[Category: tamoxifen]]
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[[Category: Tamoxifen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:12:03 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:54:49 2008''
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Revision as of 00:12, 4 May 2008

Image:2ewp.gif

Template:STRUCTURE 2ewp

Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182


Overview

The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity.

About this Structure

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

Reference

Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma., Chao EY, Collins JL, Gaillard S, Miller AB, Wang L, Orband-Miller LA, Nolte RT, McDonnell DP, Willson TM, Zuercher WJ, Bioorg Med Chem Lett. 2006 Feb 15;16(4):821-4. Epub 2005 Nov 22. PMID:16307879 Page seeded by OCA on Sun May 4 03:12:03 2008

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OCA

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