2ewp
From Proteopedia
(New page: 200px<br /> <applet load="2ewp" size="450" color="white" frame="true" align="right" spinBox="true" caption="2ewp, resolution 2.30Å" /> '''Crystal structure o...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:2ewp.gif|left|200px]]<br /> | + | [[Image:2ewp.gif|left|200px]]<br /><applet load="2ewp" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2ewp" size=" | + | |
caption="2ewp, resolution 2.30Å" /> | caption="2ewp, resolution 2.30Å" /> | ||
'''Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182'''<br /> | '''Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are | + | The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity. |
==About this Structure== | ==About this Structure== | ||
| - | 2EWP 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 TXF as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 2EWP 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=TXF:'>TXF</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2EWP OCA]. |
==Reference== | ==Reference== | ||
| Line 14: | Line 13: | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Nolte, R | + | [[Category: Nolte, R T.]] |
[[Category: TXF]] | [[Category: TXF]] | ||
[[Category: err]] | [[Category: err]] | ||
| Line 21: | Line 20: | ||
[[Category: tamoxifen]] | [[Category: tamoxifen]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:15:19 2008'' |
Revision as of 15:15, 21 February 2008
|
Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182
Overview
The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity.
About this Structure
2EWP is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
Reference
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma., Chao EY, Collins JL, Gaillard S, Miller AB, Wang L, Orband-Miller LA, Nolte RT, McDonnell DP, Willson TM, Zuercher WJ, Bioorg Med Chem Lett. 2006 Feb 15;16(4):821-4. Epub 2005 Nov 22. PMID:16307879
Page seeded by OCA on Thu Feb 21 17:15:19 2008
