2pog
From Proteopedia
(New page: 200px<br /> <applet load="2pog" size="450" color="white" frame="true" align="right" spinBox="true" caption="2pog, resolution 1.840Å" /> '''Benzopyrans as Sel...) |
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| - | [[Image:2pog. | + | [[Image:2pog.jpg|left|200px]]<br /><applet load="2pog" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2pog" size=" | + | |
caption="2pog, resolution 1.840Å" /> | caption="2pog, resolution 1.840Å" /> | ||
'''Benzopyrans as Selective Estrogen Receptor b Agonists (SERBAs). Part 2: Structure Activity Relationship Studies on the Benzopyran Scaffold.'''<br /> | '''Benzopyrans as Selective Estrogen Receptor b Agonists (SERBAs). Part 2: Structure Activity Relationship Studies on the Benzopyran Scaffold.'''<br /> | ||
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==Overview== | ==Overview== | ||
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here, we describe structure-activity relationship studies that led to the, discovery of bezopyran 5b. X-ray crystal structures of 5b and a, non-selective analog 5c in ERalpha help explain the observed selectivity, of the benzopyran platform. | Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here, we describe structure-activity relationship studies that led to the, discovery of bezopyran 5b. X-ray crystal structures of 5b and a, non-selective analog 5c in ERalpha help explain the observed selectivity, of the benzopyran platform. | ||
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| - | ==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== | ||
| - | 2POG 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 WST as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 2POG 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=WST:'>WST</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2POG OCA]. |
==Reference== | ==Reference== | ||
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[[Category: nuclear receptor]] | [[Category: nuclear receptor]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 13:40:03 2008'' |
Revision as of 11:40, 23 January 2008
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Benzopyrans as Selective Estrogen Receptor b Agonists (SERBAs). Part 2: Structure Activity Relationship Studies on the Benzopyran Scaffold.
Overview
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here, we describe structure-activity relationship studies that led to the, discovery of bezopyran 5b. X-ray crystal structures of 5b and a, non-selective analog 5c in ERalpha help explain the observed selectivity, of the benzopyran platform.
About this Structure
2POG 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 2: structure-activity relationship studies on the benzopyran scaffold., Richardson TI, Norman BH, Lugar CW, Jones SA, Wang Y, Durbin JD, Krishnan V, Dodge JA, Bioorg Med Chem Lett. 2007 Jul 1;17(13):3570-4. Epub 2007 Apr 25. PMID:17485205
Page seeded by OCA on Wed Jan 23 13:40:03 2008
