2qxm

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[[Image:2qxm.jpg|left|200px]]
[[Image:2qxm.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2qxm |SIZE=350|CAPTION= <scene name='initialview01'>2qxm</scene>, resolution 2.30&Aring;
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The line below this paragraph, containing "STRUCTURE_2qxm", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Piq+Binding+Site+For+Residue+A+1'>AC1</scene> and <scene name='pdbsite=AC2:Piq+Binding+Site+For+Residue+B+1'>AC2</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=PIQ:2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE'>PIQ</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= ESR1, ESR, NR3A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=<span class='plainlinks'>[http://www.ncbi.nlm.nih.gov/Structure/cdd/cddsrv.cgi?uid=pfam00104 Hormone_recep]</span>
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{{STRUCTURE_2qxm| PDB=2qxm | SCENE= }}
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|RELATEDENTRY=[[2qr9|2QR9]], [[2qse|2QSE]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2qxm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2qxm OCA], [http://www.ebi.ac.uk/pdbsum/2qxm PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2qxm RCSB]</span>
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}}
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'''Crystal Structure of the Estrogen Receptor Alpha Ligand Binding Domain Complexed to Burned Meat Compound PhIP'''
'''Crystal Structure of the Estrogen Receptor Alpha Ligand Binding Domain Complexed to Burned Meat Compound PhIP'''
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[[Category: Shi, Y.]]
[[Category: Shi, Y.]]
[[Category: Zhou, H.]]
[[Category: Zhou, H.]]
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[[Category: alternative splicing]]
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[[Category: Alternative splicing]]
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[[Category: dna-binding]]
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[[Category: Dna-binding]]
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[[Category: lipid-binding]]
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[[Category: Lipid-binding]]
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[[Category: metal-binding]]
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[[Category: Metal-binding]]
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[[Category: nucleus]]
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[[Category: Nucleus]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: polymorphism]]
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[[Category: Polymorphism]]
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[[Category: protein-ligand complex]]
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[[Category: Protein-ligand complex]]
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[[Category: receptor]]
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[[Category: Receptor]]
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[[Category: steroid-binding]]
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[[Category: Steroid-binding]]
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[[Category: transcription]]
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[[Category: Transcription]]
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[[Category: transcription regulation]]
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[[Category: Transcription regulation]]
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[[Category: zinc]]
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[[Category: Zinc]]
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[[Category: zinc-finger]]
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[[Category: Zinc-finger]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 15:53:02 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Apr 2 11:32:07 2008''
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Revision as of 12:53, 4 May 2008

Image:2qxm.jpg

Template:STRUCTURE 2qxm

Crystal Structure of the Estrogen Receptor Alpha Ligand Binding Domain Complexed to Burned Meat Compound PhIP


Overview

Our understanding of how steroid hormones regulate physiological functions has been significantly advanced by structural biology approaches. However, progress has been hampered by misfolding of the ligand binding domains in heterologous expression systems and by conformational flexibility that interferes with crystallization. Here, we show that protein folding problems that are common to steroid hormone receptors are circumvented by mutations that stabilize well-characterized conformations of the receptor. We use this approach to present the structure of an apo steroid receptor that reveals a ligand-accessible channel allowing soaking of preformed crystals. Furthermore, crystallization of different pharmacological classes of compounds allowed us to define the structural basis of NFkappaB-selective signaling through the estrogen receptor, thus revealing a unique conformation of the receptor that allows selective suppression of inflammatory gene expression. The ability to crystallize many receptor-ligand complexes with distinct pharmacophores allows one to define structural features of signaling specificity that would not be apparent in a single structure.

About this Structure

2QXM is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

NFkappaB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses., Nettles KW, Bruning JB, Gil G, Nowak J, Sharma SK, Hahm JB, Kulp K, Hochberg RB, Zhou H, Katzenellenbogen JA, Katzenellenbogen BS, Kim Y, Joachmiak A, Greene GL, Nat Chem Biol. 2008 Apr;4(4):241-7. Epub 2008 Mar 16. PMID:18344977 Page seeded by OCA on Sun May 4 15:53:02 2008

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