1xnn: Difference between revisions

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[[Image:1xnn.gif|left|200px]]
{{Seed}}
[[Image:1xnn.png|left|200px]]


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{{STRUCTURE_1xnn|  PDB=1xnn  |  SCENE=  }}  
{{STRUCTURE_1xnn|  PDB=1xnn  |  SCENE=  }}  


'''CRYSTAL STRUCTURE OF THE RAT ANDROGEN RECEPTOR LIGAND BINDING DOMAIN T877A MUTANT COMPLEX WITH (3A-ALPHA-,4-ALPHA 7-ALPHA-,7A-ALPHA-)-3A,4,7,7A-TETRAHYDRO-2-(4-NITRO-1-NAPHTHALENYL)-4,7-ETHANO-1H-ISOINDOLE-1,3(2H)-DIONE.'''
===CRYSTAL STRUCTURE OF THE RAT ANDROGEN RECEPTOR LIGAND BINDING DOMAIN T877A MUTANT COMPLEX WITH (3A-ALPHA-,4-ALPHA 7-ALPHA-,7A-ALPHA-)-3A,4,7,7A-TETRAHYDRO-2-(4-NITRO-1-NAPHTHALENYL)-4,7-ETHANO-1H-ISOINDOLE-1,3(2H)-DIONE.===




==Overview==
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A novel series of isoindoledione based compounds were identified as potent antagonists of the androgen receptor (AR). Co-crystallization of members of this family of inhibitors was successfully accomplished with the T877A AR LBD. A working model of how this class of compounds functions to antagonize the AR was created. Based on this model, it was proposed that expanding the bicyclic portion of the molecule should result in analogs which function as effective antagonists against a variety of AR isoforms. In contrast to what was predicted by the model, SAR around this new series was dictated by the aniline portion rather than the bicyclic portion of the molecule.
The line below this paragraph, {{ABSTRACT_PUBMED_15603938}}, adds the Publication Abstract to the page
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{{ABSTRACT_PUBMED_15603938}}


==About this Structure==
==About this Structure==
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[[Category: Steroid receptor]]
[[Category: Steroid receptor]]
[[Category: Transcription regulation]]
[[Category: Transcription regulation]]
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