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2ewp
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(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...)
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Revision as of 19:50, 12 November 2007
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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 TXF 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 Mon Nov 12 21:56:42 2007
