2iok: Difference between revisions

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New page: left|200px<br /> <applet load="2iok" size="450" color="white" frame="true" align="right" spinBox="true" caption="2iok, resolution 2.40Å" /> '''Human estrogen rece...
 
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[[Image:2iok.gif|left|200px]]<br />
[[Image:2iok.jpg|left|200px]]<br /><applet load="2iok" size="350" color="white" frame="true" align="right" spinBox="true"  
<applet load="2iok" size="450" color="white" frame="true" align="right" spinBox="true"  
caption="2iok, resolution 2.40&Aring;" />
caption="2iok, resolution 2.40&Aring;" />
'''Human estrogen receptor alpha ligand-binding domain in complex with compound 1D'''<br />
'''Human estrogen receptor alpha ligand-binding domain in complex with compound 1D'''<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.
==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==
2IOK 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 IOK as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2IOK OCA].  
2IOK 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=IOK:'>IOK</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2IOK OCA].  


==Reference==
==Reference==
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[[Category: transcription factor]]
[[Category: transcription factor]]


''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 22:46:36 2007''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:59:39 2008''
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