2qa6

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{{STRUCTURE_2qa6| PDB=2qa6 | SCENE= }}
{{STRUCTURE_2qa6| PDB=2qa6 | SCENE= }}
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'''Crystal Structure of Estrogen Receptor Alpha mutant 537S Complexed with 4-(6-hydroxy-1H-indazol-3-yl)benzene-1,3-diol'''
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===Crystal Structure of Estrogen Receptor Alpha mutant 537S Complexed with 4-(6-hydroxy-1H-indazol-3-yl)benzene-1,3-diol===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 18344977 is the PubMed ID number.
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{{ABSTRACT_PUBMED_18344977}}
==About this Structure==
==About this Structure==
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[[Category: Protein-ligand complex]]
[[Category: Protein-ligand complex]]
[[Category: Transcription]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:37:05 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 15:29:02 2008''

Revision as of 12:29, 29 July 2008

Image:2qa6.png

Template:STRUCTURE 2qa6

Crystal Structure of Estrogen Receptor Alpha mutant 537S Complexed with 4-(6-hydroxy-1H-indazol-3-yl)benzene-1,3-diol

Template:ABSTRACT PUBMED 18344977

About this Structure

2QA6 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

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