2pog
From Proteopedia
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| - | [[Image:2pog.jpg|left|200px]] | + | [[Image:2pog.jpg|left|200px]] |
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| - | '''Benzopyrans as Selective Estrogen Receptor b Agonists (SERBAs). Part 2: Structure Activity Relationship Studies on the Benzopyran Scaffold.''' | + | {{Structure |
| + | |PDB= 2pog |SIZE=350|CAPTION= <scene name='initialview01'>2pog</scene>, resolution 1.840Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=WST:(3AS,4R,9BR)-4-(4-HYDROXYPHENYL)-1,2,3,3A,4,9B-HEXAHYDROCYCLOPENTA[C]CHROMEN-9-OL'>WST</scene> | ||
| + | |ACTIVITY= | ||
| + | |GENE= ESR1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | }} | ||
| + | |||
| + | '''Benzopyrans as Selective Estrogen Receptor b Agonists (SERBAs). Part 2: Structure Activity Relationship Studies on the Benzopyran Scaffold.''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2POG is a [ | + | 2POG is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2POG OCA]. |
==Reference== | ==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:[http:// | + | 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:[http://www.ncbi.nlm.nih.gov/pubmed/17485205 17485205] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
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[[Category: nuclear receptor]] | [[Category: nuclear receptor]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:15:34 2008'' |
Revision as of 16:15, 20 March 2008
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| , resolution 1.840Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | ESR1 (Homo sapiens) | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Benzopyrans as Selective Estrogen Receptor b Agonists (SERBAs). Part 2: Structure Activity Relationship Studies on the Benzopyran Scaffold.
Contents |
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.
Disease
Known diseases associated with this structure: Atherosclerosis, susceptibility to OMIM:[133430], Breast cancer OMIM:[133430], Estrogen resistance OMIM:[133430], HDL response to hormone replacement, augmented OMIM:[133430], Migraine, susceptibility to OMIM:[133430], Myocardial infarction, susceptibility to OMIM:[133430]
About this Structure
2POG is a Single protein structure of sequence from Homo sapiens. 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 Thu Mar 20 18:15:34 2008
