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2ewp
From Proteopedia
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[[Image:2ewp.gif|left|200px]] | [[Image:2ewp.gif|left|200px]] | ||
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'''Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182''' | '''Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182''' | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Nolte, R T.]] | [[Category: Nolte, R T.]] | ||
| - | [[Category: | + | [[Category: Err]] |
| - | [[Category: | + | [[Category: Estrogen related receptor]] |
| - | [[Category: | + | [[Category: Orphan receptor]] |
| - | [[Category: | + | [[Category: Tamoxifen]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:12:03 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 00:12, 4 May 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. 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 Sun May 4 03:12:03 2008
