2z4b: Difference between revisions
New page: left|200px<br /> <applet load="2z4b" size="450" color="white" frame="true" align="right" spinBox="true" caption="2z4b, resolution 2.34Å" /> '''Estrogen receptor b... |
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[[Image:2z4b. | [[Image:2z4b.jpg|left|200px]]<br /><applet load="2z4b" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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'''Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand'''<br /> | '''Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
2Z4B 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 DC8 as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | 2Z4B 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=DC8:'>DC8</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Z4B OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: transcription]] | [[Category: transcription]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 13:32:16 2008'' | ||
Revision as of 14:32, 23 January 2008
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Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand
OverviewOverview
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here, we describe the syntheses of cyclopentanone and cyclohexanone, intermediates for SAR studies of the C-ring on the benzopyran scaffold., Modification of the C-ring disrupts binding to ERalpha, thus improving, ERbeta selectivity up to 100-fold. X-ray cocrystal structures confirm, previously observed binding modes.
About this StructureAbout this Structure
2Z4B is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
ReferenceReference
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: Synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification., Richardson TI, Dodge JA, Durst GL, Pfeifer LA, Shah J, Wang Y, Durbin JD, Krishnan V, Norman BH, Bioorg Med Chem Lett. 2007 Sep 1;17(17):4824-8. Epub 2007 Jun 20. PMID:17614275
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