2i0g
From Proteopedia
(New page: 200px<br /> <applet load="2i0g" size="450" color="white" frame="true" align="right" spinBox="true" caption="2i0g, resolution 2.500Å" /> '''Benzopyrans are Se...) |
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| - | [[Image:2i0g.gif|left|200px]]<br /> | + | [[Image:2i0g.gif|left|200px]]<br /><applet load="2i0g" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2i0g" size=" | + | |
caption="2i0g, resolution 2.500Å" /> | caption="2i0g, resolution 2.500Å" /> | ||
'''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 | + | 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. |
==About this Structure== | ==About this Structure== | ||
| - | 2I0G 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:// | + | 2I0G 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=2I0G OCA]. |
==Reference== | ==Reference== | ||
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[[Category: nuclear receptor]] | [[Category: nuclear receptor]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:47:43 2008'' |
Revision as of 15:47, 21 February 2008
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Benzopyrans are Selective Estrogen Receptor beta Agonists (SERBAs) with Novel Activity in Models of Benign Prostatic Hyperplasia
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.
About this Structure
2I0G is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
Reference
Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia., Norman BH, Dodge JA, Richardson TI, Borromeo PS, Lugar CW, Jones SA, Chen K, Wang Y, Durst GL, Barr RJ, Montrose-Rafizadeh C, Osborne HE, Amos RM, Guo S, Boodhoo A, Krishnan V, J Med Chem. 2006 Oct 19;49(21):6155-7. PMID:17034120
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