1sj0

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{{STRUCTURE_1sj0| PDB=1sj0 | SCENE= }}
{{STRUCTURE_1sj0| PDB=1sj0 | SCENE= }}
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'''Human Estrogen Receptor Alpha Ligand-binding Domain in Complex with the Antagonist Ligand 4-D'''
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===Human Estrogen Receptor Alpha Ligand-binding Domain in Complex with the Antagonist Ligand 4-D===
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==Overview==
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The discovery and synthesis of dihydrobenzoxathiins as potent, ERalpha subtype selective ligands are described. The most active analogue, 4-D, was found to be 50-fold selective in a competitive binding assay and 100-fold selective in a transactivation assay in HEK-293 cells. The alpha selectivity was postulated to lie in the interaction of the sulfur atom of the benzoxathiin ring with the two discriminating residues in the binding pocket of the receptor isoforms.
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(as it appears on PubMed at http://www.pubmed.gov), where 15084115 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15084115}}
==About this Structure==
==About this Structure==
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[[Category: Nuclear receptor]]
[[Category: Nuclear receptor]]
[[Category: Transcription factor]]
[[Category: Transcription factor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 08:45:34 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 03:12:20 2008''

Revision as of 00:12, 29 July 2008

Image:1sj0.png

Template:STRUCTURE 1sj0

Human Estrogen Receptor Alpha Ligand-binding Domain in Complex with the Antagonist Ligand 4-D

Template:ABSTRACT PUBMED 15084115

About this Structure

1SJ0 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators., Kim S, Wu JY, Birzin ET, Frisch K, Chan W, Pai LY, Yang YT, Mosley RT, Fitzgerald PM, Sharma N, Dahllund J, Thorsell AG, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML, J Med Chem. 2004 Apr 22;47(9):2171-5. PMID:15084115

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