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2z4b

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[[Image:2z4b.jpg|left|200px]]
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{{STRUCTURE_2z4b| PDB=2z4b | SCENE= }}
{{STRUCTURE_2z4b| PDB=2z4b | SCENE= }}
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'''Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand'''
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===Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand===
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==Overview==
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Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here we describe the syntheses of cyclopentanone and cyclohexanone intermediates for SAR studies of the C-ring on the benzopyran scaffold. Modification of the C-ring disrupts binding to ERalpha, thus improving ERbeta selectivity up to 100-fold. X-ray cocrystal structures confirm previously observed binding modes.
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(as it appears on PubMed at http://www.pubmed.gov), where 17614275 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17614275}}
==About this Structure==
==About this Structure==
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[[Category: Nuclear receptor ligand binding domain]]
[[Category: Nuclear receptor ligand binding domain]]
[[Category: Transcription]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 19:56:20 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 01:57:32 2008''

Revision as of 22:57, 27 July 2008

Image:2z4b.png

Template:STRUCTURE 2z4b

Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand

Template:ABSTRACT PUBMED 17614275

About this Structure

2Z4B is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification., Richardson TI, Dodge JA, Durst GL, Pfeifer LA, Shah J, Wang Y, Durbin JD, Krishnan V, Norman BH, Bioorg Med Chem Lett. 2007 Sep 1;17(17):4824-8. Epub 2007 Jun 20. PMID:17614275

Page seeded by OCA on Mon Jul 28 01:57:32 2008

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