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| {{STRUCTURE_2qa8| PDB=2qa8 | SCENE= }} | | {{STRUCTURE_2qa8| PDB=2qa8 | SCENE= }} |
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| '''Crystal Structure of the Estrogen Receptor Alpha Ligand Binding Domain Mutant 537S Complexed with Genistein'''
| | ===Crystal Structure of the Estrogen Receptor Alpha Ligand Binding Domain Mutant 537S Complexed with Genistein=== |
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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.
| | The line below this paragraph, {{ABSTRACT_PUBMED_18344977}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 18344977 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_18344977}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Protein-ligand complex]] | | [[Category: Protein-ligand complex]] |
| [[Category: Transcription]] | | [[Category: Transcription]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:37:07 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 10:38:44 2008'' |
