2ihq: Difference between revisions

New page: left|200px<br /><applet load="2ihq" size="450" color="white" frame="true" align="right" spinBox="true" caption="2ihq, resolution 2.00Å" /> '''Crystal Structure of...
 
No edit summary
Line 1: Line 1:
[[Image:2ihq.jpg|left|200px]]<br /><applet load="2ihq" size="450" color="white" frame="true" align="right" spinBox="true"  
[[Image:2ihq.jpg|left|200px]]<br /><applet load="2ihq" size="350" color="white" frame="true" align="right" spinBox="true"  
caption="2ihq, resolution 2.00&Aring;" />
caption="2ihq, resolution 2.00&Aring;" />
'''Crystal Structure of the Rat Androgen Receptor Ligand Binding Domian Complex with an N-Aryl-Hydroxybicyclohydantoin'''<br />
'''Crystal Structure of the Rat Androgen Receptor Ligand Binding Domian Complex with an N-Aryl-Hydroxybicyclohydantoin'''<br />


==Overview==
==Overview==
A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator, scaffold was discovered through structure-guided modifications of androgen, receptor antagonists. A prototype compound (7R,7aS)-10b from this series, is a potent and highly tissue-selective agonist of the androgen receptor., After oral dosing in a rat atrophied levator ani muscle model, (7R,7aS)-10b demonstrated efficacy at restoring levator ani muscle mass to, that of intact controls and exhibited &gt;50-fold selectivity for muscle over, prostate.
A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered through structure-guided modifications of androgen receptor antagonists. A prototype compound (7R,7aS)-10b from this series is a potent and highly tissue-selective agonist of the androgen receptor. After oral dosing in a rat atrophied levator ani muscle model, (7R,7aS)-10b demonstrated efficacy at restoring levator ani muscle mass to that of intact controls and exhibited &gt;50-fold selectivity for muscle over prostate.


==About this Structure==
==About this Structure==
2IHQ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with LG7 as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2IHQ OCA].  
2IHQ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with <scene name='pdbligand=LG7:'>LG7</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2IHQ OCA].  


==Reference==
==Reference==
Line 13: Line 13:
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Sack, J.S.]]
[[Category: Sack, J S.]]
[[Category: LG7]]
[[Category: LG7]]
[[Category: androgen receptor]]
[[Category: androgen receptor]]
Line 21: Line 21:
[[Category: transcription regulation]]
[[Category: transcription regulation]]


''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Wed Nov 21 12:19:31 2007''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:52:53 2008''

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA