View source for 1qku

[[Image:1qku.gif|left|200px]]<br />
<applet load="1qku" size="450" color="white" frame="true" align="right" spinBox="true" 
caption="1qku, resolution 3.20&Aring;" />
'''WILD TYPE ESTROGEN NUCLEAR RECEPTOR LIGAND BINDING DOMAIN COMPLEXED WITH ESTRADIOL'''<br />

==Overview==
The crystal structure of a triple cysteine to serine mutant ERalpha, ligand-binding domain (LBD), complexed with estradiol, shows that despite, the presence of a tightly bound agonist ligand, the protein exhibits an, antagonist-like conformation, similar to that observed in raloxifen and, 4-hydroxytamoxifen-bound structures. This mutated receptor binds estradiol, with wild type affinity and displays transcriptional activity upon, estradiol stimulation, but with limited potency (about 50%). This partial, activity is efficiently repressed in antagonist competition assays. The, comparison with available LBD structures reveals key features governing, the positioning of helix H12 and highlights the importance of cysteine, residues in promoting an active conformation. Furthermore the present, ... [[http://ispc.weizmann.ac.il/pmbin/getpm?11278577 (full description)]]

==About this Structure==
1QKU is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with EST as [[http://en.wikipedia.org/wiki/ligand ligand]]. The following page contains interesting information on the relation of 1QKU with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb45_1.html Estrogen Receptor]]. Structure known Active Sites: AC1, AC2 and AC3. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1QKU OCA]]. 

==Reference==
Crystal structure of a mutant hERalpha ligand-binding domain reveals key structural features for the mechanism of partial agonism., Gangloff M, Ruff M, Eiler S, Duclaud S, Wurtz JM, Moras D, J Biol Chem. 2001 May 4;276(18):15059-65. Epub 2001 Feb 6. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=11278577 11278577]
[[Category: Estrogen Receptor]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Duclaud, S.]]
[[Category: Eiler, S.]]
[[Category: Gangloff, M.]]
[[Category: Moras, D.]]
[[Category: Ruff, M.]]
[[Category: SPINE, Structural.Proteomics.in.Europe.]]
[[Category: Wurtz, J.M.]]
[[Category: EST]]
[[Category: agonism]]
[[Category: antagonism]]
[[Category: crystal structure]]
[[Category: estradiol receptor]]
[[Category: spine]]
[[Category: steroid]]
[[Category: structural genomics]]
[[Category: structural proteomics in europe]]

''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 10:27:57 2007''