2ewp: Difference between revisions
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|ACTIVITY= | |ACTIVITY= | ||
|GENE= ESRRG, ERR3, ERRG2, KIAA0832, NR3B3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= ESRRG, ERR3, ERRG2, KIAA0832, NR3B3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
|DOMAIN= | |||
|RELATEDENTRY= | |||
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ewp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ewp OCA], [http://www.ebi.ac.uk/pdbsum/2ewp PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ewp RCSB]</span> | |||
}} | }} | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Nolte, R T.]] | [[Category: Nolte, R T.]] | ||
[[Category: err]] | [[Category: err]] | ||
[[Category: estrogen related receptor]] | [[Category: estrogen related receptor]] | ||
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[[Category: tamoxifen]] | [[Category: tamoxifen]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:54:49 2008'' | ||
Revision as of 02:54, 31 March 2008
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| , resolution 2.30Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | ESRRG, ERR3, ERRG2, KIAA0832, NR3B3 (Homo sapiens) | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182
OverviewOverview
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 StructureAbout this Structure
2EWP is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
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
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