2giu

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(New page: 200px<br /> <applet load="2giu" size="450" color="white" frame="true" align="right" spinBox="true" caption="2giu, resolution 2.2&Aring;" /> '''Human estrogen recep...)
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Revision as of 20:12, 12 November 2007

Image:2giu.gif

2giu, resolution 2.2Å

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Human estrogen receptor beta ligand-binding domain in complex with compound 45

Overview

Synthesis and derivatization of a series of substituted, tetrahydrofluorenone analogs giving potent, ERbeta subtype selective, ligands are described. Several analogs possessing ERbeta binding, affinities comparable to 17beta-estradiol but with greater than 75-fold, selectivity over ERalpha are reported.

About this Structure

2GIU is a Single protein structure of sequence from Homo sapiens with FBR as ligand. Full crystallographic information is available from OCA.

Reference

The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands., Wilkening RR, Ratcliffe RW, Tynebor EC, Wildonger KJ, Fried AK, Hammond ML, Mosley RT, Fitzgerald PM, Sharma N, McKeever BM, Nilsson S, Carlquist M, Thorsell A, Locco L, Katz R, Frisch K, Birzin ET, Wilkinson HA, Mitra S, Cai S, Hayes EC, Schaeffer JM, Rohrer SP, Bioorg Med Chem Lett. 2006 Jul 1;16(13):3489-94. Epub 2006 May 2. PMID:16632357

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