1qkm: Difference between revisions

Revision as of 06:23, 3 May 2008

HUMAN OESTROGEN RECEPTOR BETA LIGAND-BINDING DOMAIN IN COMPLEX WITH PARTIAL AGONIST GENISTEIN

OverviewOverview

Oestrogens exert their physiological effects through two receptor subtypes. Here we report the three-dimensional structure of the oestrogen receptor beta isoform (ERbeta) ligand-binding domain (LBD) in the presence of the phyto-oestrogen genistein and the antagonist raloxifene. The overall structure of ERbeta-LBD is very similar to that previously reported for ERalpha. Each ligand interacts with a unique set of residues within the hormone-binding cavity and induces a distinct orientation in the AF-2 helix (H12). The bulky side chain of raloxifene protrudes from the cavity and physically prevents the alignment of H12 over the bound ligand. In contrast, genistein is completely buried within the hydrophobic core of the protein and binds in a manner similar to that observed for ER's endogenous hormone, 17beta-oestradiol. However, in the ERbeta-genistein complex, H12 does not adopt the distinctive 'agonist' position but, instead, lies in a similar orientation to that induced by ER antagonists. Such a sub-optimal alignment of the transactivation helix is consistent with genistein's partial agonist character in ERbeta and demonstrates how ER's transcriptional response to certain bound ligands is attenuated.

About this StructureAbout this Structure

1QKM is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Structure of the ligand-binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist., Pike AC, Brzozowski AM, Hubbard RE, Bonn T, Thorsell AG, Engstrom O, Ljunggren J, Gustafsson JA, Carlquist M, EMBO J. 1999 Sep 1;18(17):4608-18. PMID:10469641 Page seeded by OCA on Sat May 3 06:23:17 2008

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OCA

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 [[Image:1qkm.gif|left|200px]]
- {{Structure
+<!--
-|PDB= 1qkm |SIZE=350|CAPTION= <scene name='initialview01'>1qkm</scene>, resolution 1.8&Aring;
+The line below this paragraph, containing "STRUCTURE_1qkm", 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=GEN:GENISTEIN'>GEN</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= OESTROGEN RECEPTOR BETA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+-->
-|DOMAIN=
+{{STRUCTURE_1qkm|  PDB=1qkm  |  SCENE=  }}
-|RELATEDENTRY=
-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1qkm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1qkm OCA], [http://www.ebi.ac.uk/pdbsum/1qkm PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1qkm RCSB]</span>
-}}
 '''HUMAN OESTROGEN RECEPTOR BETA LIGAND-BINDING DOMAIN IN COMPLEX WITH PARTIAL AGONIST GENISTEIN'''
@@ Line 28: / Line 25: @@
 [[Category: Carlquist, M.]]
 [[Category: Pike, A C.W.]]
-[[Category: nuclear receptor]]
+[[Category: Nuclear receptor]]
-[[Category: partial agonist]]
+[[Category: Partial agonist]]
-[[Category: phyto-oestrogen]]
+[[Category: Phyto-oestrogen]]
-[[Category: transcription factor]]
+[[Category: Transcription factor]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 06:23:17 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:15:01 2008''