2ewp: Difference between revisions

Revision as of 03:12, 4 May 2008

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 Page seeded by OCA on Sun May 4 03:12:03 2008

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

@@ Line 1: / Line 1: @@
 [[Image:2ewp.gif|left|200px]]
- {{Structure
+<!--
-|PDB= 2ewp |SIZE=350|CAPTION= <scene name='initialview01'>2ewp</scene>, resolution 2.30&Aring;
+The line below this paragraph, containing "STRUCTURE_2ewp", creates the "Structure Box" on the page.
-|SITE=
+You may change the PDB parameter (which sets the PDB file loaded into the applet)
-|LIGAND= <scene name='pdbligand=TXF:(Z)-4-(1-{4-[2-(DIMETHYLAMINO)ETHOXY]PHENYL}-5-HYDROXY-2-PHENYLPENT-1-ENYL)PHENOL'>TXF</scene>
+or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-|ACTIVITY=
+or leave the SCENE parameter empty for the default display.
-|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=
+{{STRUCTURE_2ewp|  PDB=2ewp  |  SCENE=  }}
-|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>
-}}
 '''Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182'''
@@ Line 26: / Line 23: @@
 [[Category: Single protein]]
 [[Category: Nolte, R T.]]
-[[Category: err]]
+[[Category: Err]]
-[[Category: estrogen related receptor]]
+[[Category: Estrogen related receptor]]
-[[Category: orphan receptor]]
+[[Category: Orphan receptor]]
-[[Category: tamoxifen]]
+[[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 Mon Mar 31 02:54:49 2008''