2i0j: Difference between revisions

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New page: left|200px<br /> <applet load="2i0j" size="450" color="white" frame="true" align="right" spinBox="true" caption="2i0j, resolution 2.900Å" /> '''Benzopyrans are Se...
 
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[[Image:2i0j.gif|left|200px]]<br />
[[Image:2i0j.gif|left|200px]]<br /><applet load="2i0j" size="350" color="white" frame="true" align="right" spinBox="true"  
<applet load="2i0j" size="450" color="white" frame="true" align="right" spinBox="true"  
caption="2i0j, resolution 2.900&Aring;" />
caption="2i0j, resolution 2.900&Aring;" />
'''Benzopyrans are Selective Estrogen Receptor beta Agonists (SERBAs) with Novel Activity in Models of Benign Prostatic Hyperplasia'''<br />
'''Benzopyrans are Selective Estrogen Receptor beta Agonists (SERBAs) with Novel Activity in Models of Benign Prostatic Hyperplasia'''<br />


==Overview==
==Overview==
Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows, potent, selective binding and agonist function in estrogen receptor beta, (ERbeta) in vitro assays. X-ray crystal structures of SERBA-1 in ERalpha, and beta help explain observed beta-selectivity of this ligand. SERBA-1 in, vivo demonstrates involution of the ventral prostate in CD-1 mice (ERbeta, effect), while having no effect on gonadal hormone levels (ERalpha effect), at 10x the efficacious dose, consistent with in vitro properties of this, molecule.
Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows potent, selective binding and agonist function in estrogen receptor beta (ERbeta) in vitro assays. X-ray crystal structures of SERBA-1 in ERalpha and beta help explain observed beta-selectivity of this ligand. SERBA-1 in vivo demonstrates involution of the ventral prostate in CD-1 mice (ERbeta effect), while having no effect on gonadal hormone levels (ERalpha effect) at 10x the efficacious dose, consistent with in vitro properties of this molecule.


==Disease==
==Disease==
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==About this Structure==
==About this Structure==
2I0J 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 I0G as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2I0J OCA].  
2I0J 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=I0G:'>I0G</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2I0J OCA].  


==Reference==
==Reference==
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[[Category: nuclear receptor ligand binding domain]]
[[Category: nuclear receptor ligand binding domain]]


''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 22:39:25 2007''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:47:45 2008''