2p15

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[[Image:2p15.gif|left|200px]]
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{{STRUCTURE_2p15| PDB=2p15 | SCENE= }}
{{STRUCTURE_2p15| PDB=2p15 | SCENE= }}
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'''Crystal structure of the ER alpha ligand binding domain with the agonist ortho-trifluoromethylphenylvinyl estradiol'''
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===Crystal structure of the ER alpha ligand binding domain with the agonist ortho-trifluoromethylphenylvinyl estradiol===
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==Overview==
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The steroid hormone receptors are characterized by binding to relatively rigid, inflexible endogenous steroid ligands. Other members of the nuclear receptor superfamily bind to conformationally flexible lipids and show a corresponding degree of elasticity in the ligand-binding pocket. Here, we report the X-ray crystal structure of the oestrogen receptor alpha (ERalpha) bound to an oestradiol derivative with a prosthetic group, ortho- trifluoromethlyphenylvinyl, which binds in a novel extended pocket in the ligand-binding domain. Unlike ER antagonists with bulky side groups, this derivative is enclosed in the ligand-binding pocket, and acts as a potent agonist. This work shows that steroid hormone receptors can interact with a wider array of pharmacophores than previously thought through structural plasticity in the ligand-binding pocket.
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(as it appears on PubMed at http://www.pubmed.gov), where 17468738 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17468738}}
==About this Structure==
==About this Structure==
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[[Category: Ligand binding domain]]
[[Category: Ligand binding domain]]
[[Category: Nulear receptor]]
[[Category: Nulear receptor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 12:07:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 20:35:43 2008''

Revision as of 17:35, 27 July 2008

Image:2p15.png

Template:STRUCTURE 2p15

Crystal structure of the ER alpha ligand binding domain with the agonist ortho-trifluoromethylphenylvinyl estradiol

Template:ABSTRACT PUBMED 17468738

About this Structure

2P15 is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural plasticity in the oestrogen receptor ligand-binding domain., Nettles KW, Bruning JB, Gil G, O'Neill EE, Nowak J, Guo Y, Kim Y, DeSombre ER, Dilis R, Hanson RN, Joachimiak A, Greene GL, EMBO Rep. 2007 Jun;8(6):563-8. Epub 2007 Apr 27. PMID:17468738

Page seeded by OCA on Sun Jul 27 20:35:43 2008

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