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New page: left|200px<br /> <applet load="1zaf" size="450" color="white" frame="true" align="right" spinBox="true" caption="1zaf, resolution 2.20Å" /> '''Crystal structure o... |
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[[Image:1zaf.gif|left|200px]]<br /> | [[Image:1zaf.gif|left|200px]]<br /><applet load="1zaf" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="1zaf" size=" | |||
caption="1zaf, resolution 2.20Å" /> | caption="1zaf, resolution 2.20Å" /> | ||
'''Crystal structure of estrogen receptor beta complexed with 3-Bromo-6-hydroxy-2-(4-hydroxy-phenyl)-inden-1-one'''<br /> | '''Crystal structure of estrogen receptor beta complexed with 3-Bromo-6-hydroxy-2-(4-hydroxy-phenyl)-inden-1-one'''<br /> | ||
==Overview== | ==Overview== | ||
The syntheses of a series of 2-arylindene-1-ones as potent ligands of | The syntheses of a series of 2-arylindene-1-ones as potent ligands of ERbeta and ERalpha are described. Several compounds exhibited high potency and moderate selectivity for the ERbeta receptor. X-ray and modeling studies were used to understand ligand binding orientation and observed affinity. | ||
==About this Structure== | ==About this Structure== | ||
1ZAF is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with 789 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] Full crystallographic information is available from [http:// | 1ZAF is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=789:'>789</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1ZAF OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Harris, H | [[Category: Harris, H A.]] | ||
[[Category: Malamas, M | [[Category: Malamas, M S.]] | ||
[[Category: Manas, E | [[Category: Manas, E S.]] | ||
[[Category: McDevitt, R | [[Category: McDevitt, R E.]] | ||
[[Category: Miller, C | [[Category: Miller, C P.]] | ||
[[Category: Unwalla, R | [[Category: Unwalla, R J.]] | ||
[[Category: Xu, Z | [[Category: Xu, Z B.]] | ||
[[Category: 789]] | [[Category: 789]] | ||
[[Category: agonist]] | [[Category: agonist]] | ||
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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 16:13:39 2008'' | ||
Revision as of 17:13, 21 February 2008
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Crystal structure of estrogen receptor beta complexed with 3-Bromo-6-hydroxy-2-(4-hydroxy-phenyl)-inden-1-one
OverviewOverview
The syntheses of a series of 2-arylindene-1-ones as potent ligands of ERbeta and ERalpha are described. Several compounds exhibited high potency and moderate selectivity for the ERbeta receptor. X-ray and modeling studies were used to understand ligand binding orientation and observed affinity.
About this StructureAbout this Structure
1ZAF is a Protein complex structure of sequences from Homo sapiens with as ligand. Active as Histone acetyltransferase, with EC number 2.3.1.48 Full crystallographic information is available from OCA.
ReferenceReference
Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones., McDevitt RE, Malamas MS, Manas ES, Unwalla RJ, Xu ZB, Miller CP, Harris HA, Bioorg Med Chem Lett. 2005 Jun 15;15(12):3137-42. PMID:15876535
Page seeded by OCA on Thu Feb 21 16:13:39 2008