2giu
From Proteopedia
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| - | [[Image:2giu.gif|left|200px]] | + | [[Image:2giu.gif|left|200px]] |
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| - | '''Human estrogen receptor beta ligand-binding domain in complex with compound 45''' | + | {{Structure |
| + | |PDB= 2giu |SIZE=350|CAPTION= <scene name='initialview01'>2giu</scene>, resolution 2.2Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=FBR:(9aS)-4-bromo-9a-butyl-7-hydroxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one'>FBR</scene> | ||
| + | |ACTIVITY= | ||
| + | |GENE= ESR2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | }} | ||
| + | |||
| + | '''Human estrogen receptor beta ligand-binding domain in complex with compound 45''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2GIU is a [ | + | 2GIU is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GIU OCA]. |
==Reference== | ==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:[http:// | + | 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:[http://www.ncbi.nlm.nih.gov/pubmed/16632357 16632357] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
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[[Category: transcription factor]] | [[Category: transcription factor]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:05:10 2008'' |
Revision as of 15:05, 20 March 2008
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| , resolution 2.2Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | ESR2 (Homo sapiens) | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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. 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
Page seeded by OCA on Thu Mar 20 17:05:10 2008
