1nde

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[[Image:1nde.gif|left|200px]]
[[Image:1nde.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1nde |SIZE=350|CAPTION= <scene name='initialview01'>1nde</scene>, resolution 3.0&Aring;
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The line below this paragraph, containing "STRUCTURE_1nde", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=MON:4-(2-{[4-{[3-(4-CHLOROPHENYL)PROPYL]SULFANYL}-6-(1-PIPERAZINYL)-1,3,5-TRIAZIN-2-YL]AMINO}ETHYL)PHENOL'>MON</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= ESTRB ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1nde| PDB=1nde | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1nde FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1nde OCA], [http://www.ebi.ac.uk/pdbsum/1nde PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1nde RCSB]</span>
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}}
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'''Estrogen Receptor beta with Selective Triazine Modulator'''
'''Estrogen Receptor beta with Selective Triazine Modulator'''
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[[Category: Williams, S P.]]
[[Category: Williams, S P.]]
[[Category: Wisely, G B.]]
[[Category: Wisely, G B.]]
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[[Category: er]]
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[[Category: Er]]
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[[Category: erb]]
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[[Category: Erb]]
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[[Category: estradiol]]
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[[Category: Estradiol]]
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[[Category: estrogen]]
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[[Category: Estrogen]]
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[[Category: estrogen receptor]]
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[[Category: Estrogen receptor]]
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[[Category: estrogen receptor beta]]
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[[Category: Estrogen receptor beta]]
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[[Category: oestrogen]]
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[[Category: Oestrogen]]
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[[Category: triazine]]
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[[Category: Triazine]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 02:23:58 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:28:50 2008''
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Revision as of 23:23, 2 May 2008

Image:1nde.gif

Template:STRUCTURE 1nde

Estrogen Receptor beta with Selective Triazine Modulator


Overview

A series of 1,3,5-triazine-based estrogen receptor (ER) modulators that are modestly selective for the ERbeta subtype are reported. Compound 1, which displayed modest potency and selectivity for ERbeta vs ERalpha, was identified via high-throughput screening utilizing an ERbeta SPA-based binding assay. Subsequent analogue preparation resulted in the identification of compounds such as 21 and 43 that display 25- to 30-fold selectivity for ERbeta with potencies in the 10-30 nM range. These compounds profile as full antagonists at ERbeta and weak partial agonists at ERalpha in a cell-based reporter gene assay. In addition, the X-ray crystal structure of compound 15 complexed with the ligand binding domain of ERbeta has been solved and was utilized in the design of more conformationally restrained analogues such as 31 in an attempt to increase selectivity for the ERbeta subtype.

About this Structure

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

Reference

A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta., Henke BR, Consler TG, Go N, Hale RL, Hohman DR, Jones SA, Lu AT, Moore LB, Moore JT, Orband-Miller LA, Robinett RG, Shearin J, Spearing PK, Stewart EL, Turnbull PS, Weaver SL, Williams SP, Wisely GB, Lambert MH, J Med Chem. 2002 Dec 5;45(25):5492-505. PMID:12459017 Page seeded by OCA on Sat May 3 02:23:58 2008

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OCA

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