2iog
From Proteopedia
(New page: 200px<br /> <applet load="2iog" size="450" color="white" frame="true" align="right" spinBox="true" caption="2iog, resolution 1.60Å" /> '''Human estrogen rece...) |
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| - | [[Image:2iog.gif|left|200px]]<br /> | + | [[Image:2iog.gif|left|200px]]<br /><applet load="2iog" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2iog" size=" | + | |
caption="2iog, resolution 1.60Å" /> | caption="2iog, resolution 1.60Å" /> | ||
'''Human estrogen receptor alpha ligand-binding domain in complex with compound 11F'''<br /> | '''Human estrogen receptor alpha ligand-binding domain in complex with compound 11F'''<br /> | ||
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==Overview== | ==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. | 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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| - | ==Disease== | ||
| - | Known diseases associated with this structure: Atherosclerosis, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=133430 133430]], Breast cancer OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=133430 133430]], Estrogen resistance OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=133430 133430]], HDL response to hormone replacement, augmented OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=133430 133430]], Migraine, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=133430 133430]], Myocardial infarction, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=133430 133430]] | ||
==About this Structure== | ==About this Structure== | ||
| - | 2IOG 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 IOG as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 2IOG 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=IOG:'>IOG</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2IOG OCA]. |
==Reference== | ==Reference== | ||
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[[Category: transcription factor]] | [[Category: transcription factor]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:59:36 2008'' |
Revision as of 10:59, 23 January 2008
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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 with as ligand. 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 Wed Jan 23 12:59:36 2008
