2giu
From Proteopedia
(New page: 200px<br /> <applet load="2giu" size="450" color="white" frame="true" align="right" spinBox="true" caption="2giu, resolution 2.2Å" /> '''Human estrogen recep...) |
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| - | [[Image:2giu.gif|left|200px]]<br /> | + | [[Image:2giu.gif|left|200px]]<br /><applet load="2giu" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2giu" size=" | + | |
caption="2giu, resolution 2.2Å" /> | caption="2giu, resolution 2.2Å" /> | ||
'''Human estrogen receptor beta ligand-binding domain in complex with compound 45'''<br /> | '''Human estrogen receptor beta ligand-binding domain in complex with compound 45'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Synthesis and derivatization of a series of substituted | + | Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported. |
==About this Structure== | ==About this Structure== | ||
| - | 2GIU 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 FBR as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 2GIU 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=FBR:'>FBR</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GIU OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Fitzgerald, P | + | [[Category: Fitzgerald, P M.D.]] |
[[Category: Sharma, N.]] | [[Category: Sharma, N.]] | ||
[[Category: FBR]] | [[Category: FBR]] | ||
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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 Thu Feb 21 17:32:05 2008'' |
Revision as of 15:32, 21 February 2008
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Human estrogen receptor beta ligand-binding domain in complex with compound 45
Overview
Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.
About this Structure
2GIU is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
Reference
The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands., Wilkening RR, Ratcliffe RW, Tynebor EC, Wildonger KJ, Fried AK, Hammond ML, Mosley RT, Fitzgerald PM, Sharma N, McKeever BM, Nilsson S, Carlquist M, Thorsell A, Locco L, Katz R, Frisch K, Birzin ET, Wilkinson HA, Mitra S, Cai S, Hayes EC, Schaeffer JM, Rohrer SP, Bioorg Med Chem Lett. 2006 Jul 1;16(13):3489-94. Epub 2006 May 2. PMID:16632357
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