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2qtu
From Proteopedia
(New page: 200px<br /> <applet load="2qtu" size="450" color="white" frame="true" align="right" spinBox="true" caption="2qtu, resolution 2.53Å" /> '''Estrogen receptor b...) |
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| - | [[Image:2qtu.gif|left|200px]]<br /> | + | [[Image:2qtu.gif|left|200px]]<br /><applet load="2qtu" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2qtu" size=" | + | |
caption="2qtu, resolution 2.53Å" /> | caption="2qtu, resolution 2.53Å" /> | ||
'''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== | ||
| - | 2QTU 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 3AS as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 2QTU 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=3AS:'>3AS</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2QTU OCA]. |
==Reference== | ==Reference== | ||
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[[Category: zinc-finger]] | [[Category: zinc-finger]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:37:52 2008'' |
Revision as of 10:37, 23 January 2008
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Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand
Overview
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here, we describe the synthesis of a late stage intermediate that allowed us to, combine A-ring and C-ring modifications and carry out simultaneous SAR, studies at both positions. Modification of both positions proved additive, maintaining affinity and improving ERbeta selectivity up to 83-fold. An, X-ray cocrystal structure confirms the previously observed binding mode in, ERbeta.
About this Structure
2QTU is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
Reference
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies., Richardson TI, Dodge JA, Wang Y, Durbin JD, Krishnan V, Norman BH, Bioorg Med Chem Lett. 2007 Oct 15;17(20):5563-6. Epub 2007 Aug 11. PMID:17804226
Page seeded by OCA on Wed Jan 23 12:37:52 2008
Categories: Homo sapiens | Single protein | Dodge, J.A. | Durbin, J.D. | Krishnan, V. | Norman, B.H. | Richardson, T.I. | Wang, Y. | 3AS | Alternative splicing | Dna-binding | Ligand-binding domain | Lipid-binding | Metal-binding | Nuclear receptor | Nucleus | Phosphorylation | Steroid-binding | Transcription | Transcription regulation | Transcription regulator | Zinc | Zinc-finger
