1l2j: Difference between revisions

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[[Image:1l2j.~~gif~~|left|200px]]

[[Image:1l2j.png|left|200px]]

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~~'''~~Human Estrogen Receptor beta Ligand-binding Domain in Complex with (R,R)-5,11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol~~'''~~

===Human Estrogen Receptor beta Ligand-binding Domain in Complex with (R,R)-5,11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol===

~~==Overview==~~

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The ~~R,R enantiomer of 5~~,~~11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2~~,~~8-diol (THC) exerts opposite effects on~~ the ~~transcriptional activity of~~ the ~~two estrogen receptor~~ (~~ER) subtypes, ER alpha and ER beta~~. ~~THC acts as an ER alpha agonist and as an ER beta antagonist~~. ~~We have determined the crystal structures of the ER alpha ligand binding domain (LBD~~) ~~bound to both THC and a fragment of the transcriptional coactivator GRIP1~~, ~~and~~ the ER beta LBD bound to THC. THC stabilizes a conformation of the ER alpha LBD that permits coactivator association and a conformation of the ER beta LBD that prevents coactivator association. A comparison of the two structures, taken together with functional data, reveals that THC does not act on ER beta through the same mechanisms used by other known ER antagonists. Instead, THC antagonizes ER beta through a novel mechanism we term 'passive antagonism'.

The line below this paragraph, {{ABSTRACT_PUBMED_11953755}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 11953755 is the PubMed ID number.

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==About this Structure==

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[[Category: Nuclear receptor]]

[[Category: Transcription factor]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Fri May~~ 2 23:28:09 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 11:33:19 2008''

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-[[Image:1l2j.gif|left|200px]]
+{{Seed}}
+[[Image:1l2j.png|left|200px]]
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 {{STRUCTURE_1l2j|  PDB=1l2j  |  SCENE=  }}
-'''Human Estrogen Receptor beta Ligand-binding Domain in Complex with (R,R)-5,11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol'''
+===Human Estrogen Receptor beta Ligand-binding Domain in Complex with (R,R)-5,11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol===
-==Overview==
+<!--
-The R,R enantiomer of 5,11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol (THC) exerts opposite effects on the transcriptional activity of the two estrogen receptor (ER) subtypes, ER alpha and ER beta. THC acts as an ER alpha agonist and as an ER beta antagonist. We have determined the crystal structures of the ER alpha ligand binding domain (LBD) bound to both THC and a fragment of the transcriptional coactivator GRIP1, and the ER beta LBD bound to THC. THC stabilizes a conformation of the ER alpha LBD that permits coactivator association and a conformation of the ER beta LBD that prevents coactivator association. A comparison of the two structures, taken together with functional data, reveals that THC does not act on ER beta through the same mechanisms used by other known ER antagonists. Instead, THC antagonizes ER beta through a novel mechanism we term 'passive antagonism'.
+The line below this paragraph, {{ABSTRACT_PUBMED_11953755}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 11953755 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_11953755}}
 ==About this Structure==
@@ Line 35: / Line 39: @@
 [[Category: Nuclear receptor]]
 [[Category: Transcription factor]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May  2 23:28:09 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul  2 11:33:19 2008''