2iog

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[[Image:2iog.gif|left|200px]]
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{{Seed}}
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[[Image:2iog.png|left|200px]]
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{{STRUCTURE_2iog| PDB=2iog | SCENE= }}
{{STRUCTURE_2iog| PDB=2iog | SCENE= }}
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'''Human estrogen receptor alpha ligand-binding domain in complex with compound 11F'''
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===Human estrogen receptor alpha ligand-binding domain in complex with compound 11F===
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==Overview==
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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.
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The line below this paragraph, {{ABSTRACT_PUBMED_17289385}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 17289385 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17289385}}
==About this Structure==
==About this Structure==
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[[Category: Nuclear receptor]]
[[Category: Nuclear receptor]]
[[Category: Transcription factor]]
[[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 Sun Jul 27 22:38:33 2008''

Revision as of 19:38, 27 July 2008

Image:2iog.png

Template:STRUCTURE 2iog

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

Template:ABSTRACT PUBMED 17289385

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 Jul 27 22:38:33 2008

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