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2ewp

From Proteopedia

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[[Image:2ewp.gif|left|200px]]
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{{STRUCTURE_2ewp| PDB=2ewp | SCENE= }}
{{STRUCTURE_2ewp| PDB=2ewp | SCENE= }}
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'''Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182'''
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===Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 16307879 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16307879}}
==About this Structure==
==About this Structure==
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[[Category: Orphan receptor]]
[[Category: Orphan receptor]]
[[Category: Tamoxifen]]
[[Category: Tamoxifen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:12:03 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 14:25:41 2008''

Revision as of 11:25, 28 July 2008

Image:2ewp.png

Template:STRUCTURE 2ewp

Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182

Template:ABSTRACT PUBMED 16307879

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 Mon Jul 28 14:25:41 2008

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