2iog

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[[Image:2iog.gif|left|200px]]
[[Image:2iog.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2iog |SIZE=350|CAPTION= <scene name='initialview01'>2iog</scene>, resolution 1.60&Aring;
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The line below this paragraph, containing "STRUCTURE_2iog", 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=IOG:N-[(1R)-3-(4-HYDROXYPHENYL)-1-METHYLPROPYL]-2-[2-PHENYL-6-(2-PIPERIDIN-1-YLETHOXY)-1H-INDOL-3-YL]ACETAMIDE'>IOG</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_2iog| PDB=2iog | SCENE= }}
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|RELATEDENTRY=[[2iok|2IOK]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2iog FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2iog OCA], [http://www.ebi.ac.uk/pdbsum/2iog PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2iog RCSB]</span>
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}}
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'''Human estrogen receptor alpha ligand-binding domain in complex with compound 11F'''
'''Human estrogen receptor alpha ligand-binding domain in complex with compound 11F'''
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[[Category: Fitzgerald, P M.D.]]
[[Category: Fitzgerald, P M.D.]]
[[Category: Sharma, N.]]
[[Category: Sharma, N.]]
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[[Category: antagonist]]
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[[Category: Antagonist]]
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[[Category: er-alpha]]
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[[Category: Er-alpha]]
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[[Category: hormone]]
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[[Category: Hormone]]
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[[Category: nuclear receptor]]
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[[Category: Nuclear receptor]]
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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 Sun May 4 07:43:14 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:46:48 2008''
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Revision as of 04:43, 4 May 2008

Image:2iog.gif

Template:STRUCTURE 2iog

Human estrogen receptor alpha ligand-binding domain in complex with compound 11F


Overview

A novel class of indole ligands for estrogen receptor alpha have been discovered which exhibit potent affinity and high selectivity. Substitution of the bazedoxifene skeleton to the linker present in the HTS lead 1a provided 22b which was found to be 130-fold alpha-selective and acted as an antagonist of estradiol activity in uterine tissue and MCF-7 cancer cells.

About this Structure

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

Reference

Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha., Dykstra KD, Guo L, Birzin ET, Chan W, Yang YT, Hayes EC, DaSilva CA, Pai LY, Mosley RT, Kraker B, Fitzgerald PM, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML, Bioorg Med Chem Lett. 2007 Apr 15;17(8):2322-8. Epub 2007 Jan 25. PMID:17289385 Page seeded by OCA on Sun May 4 07:43:14 2008

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OCA

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