1yye - Revision history

OCA at 09:01, 14 February 2024

2024-02-14T09:01:08Z

←Older revision		Revision as of 09:01, 14 February 2024
Line 3:		Line 3:
	<StructureSection load='1yye' size='340' side='right'caption='[[1yye]], [[Resolution\|resolution]] 2.03Å' scene=''>		<StructureSection load='1yye' size='340' side='right'caption='[[1yye]], [[Resolution\|resolution]] 2.03Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[1yye]] is a 4 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1YYE OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=1YYE FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[1yye]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1YYE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1YYE FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<scene name='pdbligand=196:3~~-~~(3-FLUORO-4-HYDROXYPHENYL)-7-HYDROXY-1-NAPHTHONITRILE'>196</scene>~~</td></tr>	+	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution\|Resolution]] 2.03Å</td></tr>
-	<tr id='~~related~~'><td class="sblockLbl"><b>[[~~Related_structure~~\|~~Related~~:]]</b></td><td class="sblockDat"><~~div style~~='~~overflow~~: ~~auto; max~~-~~height: 3em;~~'>~~[[1yy4\|1yy4]]~~</~~div~~>~~</td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=196:3-(3-FLUORO-4-HYDROXYPHENYL)-7-HYDROXY-1-NAPHTHONITRILE'>196</scene></td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ESR2, ESTRB, NR3A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])~~</td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1yye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yye OCA], [https://pdbe.org/1yye PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1yye RCSB], [https://www.ebi.ac.uk/pdbsum/1yye PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1yye ProSAT]</span></td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://proteopedia.org/fgij/fg.htm?mol=1yye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yye OCA], [~~http~~://pdbe.org/1yye PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=1yye RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/1yye PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=1yye ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/ESR2_HUMAN ESR2_HUMAN]] Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.	+	[https://www.uniprot.org/uniprot/ESR2_HUMAN ESR2_HUMAN] Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 21:		Line 20:
	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1yye ConSurf].		</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1yye ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
-	<div style="background-color:#fffaf0;">
-	== Publication Abstract from PubMed ==
-	The 2-phenylnaphthalene scaffold was explored as a simplified version of genistein in order to identify ER selective ligands. With the aid of docking studies, positions 1, 4, and 8 of the 2-phenylnaphthalene template were predicted to be the most potentially influential positions to enhance ER selectivity using two different binding orientations. Both orientations have the phenol moiety mimicking the A-ring of genistein. Several compounds predicted to adopt orientations similar to that of genistein when bound to ERbeta were observed to have slightly higher ER affinity and selectivity than genistein. The second orientation we exploited, which was different from that of genistein when bound to ERbeta, resulted in the discovery of several compounds that had superior ER selectivity and affinity versus genistein. X-ray structures of two ER selective compounds (i.e., 15 and 47) confirmed the alternate binding mode and suggested that substituents at positions 1 and 8 were responsible for inducing selectivity. One compound (i.e., 47, WAY-202196) was further examined and found to be effective in two models of inflammation, suggesting that targeting ER may be therapeutically useful in treating certain chronic inflammatory diseases.
-
-	ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.,Mewshaw RE, Edsall RJ Jr, Yang C, Manas ES, Xu ZB, Henderson RA, Keith JC Jr, Harris HA J Med Chem. 2005 Jun 16;48(12):3953-79. PMID:15943471<ref>PMID:15943471</ref>
-
-	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	</div>
-	<div class="pdbe-citations 1yye" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
	*[[Estrogen receptor 3D structures\|Estrogen receptor 3D structures]]		*[[Estrogen receptor 3D structures\|Estrogen receptor 3D structures]]
-	== References ==
-	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Edsall~~, R J~~]]	+	[[Category: Edsall Jr RJ]]
-	[[Category: Harris~~, H A~~]]	+	[[Category: Harris HA]]
-	[[Category: Henderson~~, R A~~]]	+	[[Category: Henderson RA]]
-	[[Category: Keith~~, J C~~]]	+	[[Category: Keith Jr JC]]
-	[[Category: Manas~~, E S~~]]	+	[[Category: Manas ES]]
-	[[Category: Mewshaw~~, R E~~]]	+	[[Category: Mewshaw RE]]
-	[[Category: Xu~~, Z B~~]]	+	[[Category: Xu ZB]]
-	[[Category: Yang, C]]	+	[[Category: Yang C]]
-	~~[[Category: Agonist]]~~	+
-	~~[[Category: Er]]~~	+
-	~~[[Category: Er-beta]]~~	+
-	~~[[Category: Estrogen]]~~	+
-	~~[[Category: Estrogen receptor]]~~	+
-	~~[[Category: Estrogen receptor beta]]~~	+
-	~~[[Category: Nuclear receptor]]~~	+
-	~~[[Category: Transcription]]~~	+
-	~~[[Category: Transcription factor~~]]	+

OCA at 08:55, 20 January 2021

2021-01-20T08:55:20Z

←Older revision		Revision as of 08:55, 20 January 2021
Line 1:		Line 1:

	==Crystal structure of estrogen receptor beta complexed with way-202196==		==Crystal structure of estrogen receptor beta complexed with way-202196==
-	<StructureSection load='1yye' size='340' side='right' caption='[[1yye]], [[Resolution\|resolution]] 2.03Å' scene=''>	+	<StructureSection load='1yye' size='340' side='right'caption='[[1yye]], [[Resolution\|resolution]] 2.03Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[1yye]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1YYE OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=1YYE FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[1yye]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1YYE OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=1YYE FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=196:3-(3-FLUORO-4-HYDROXYPHENYL)-7-HYDROXY-1-NAPHTHONITRILE'>196</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=196:3-(3-FLUORO-4-HYDROXYPHENYL)-7-HYDROXY-1-NAPHTHONITRILE'>196</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1yy4\|1yy4]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1yy4\|1yy4]]</div></td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ESR2, ESTRB, NR3A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ESR2, ESTRB, NR3A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=1yye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yye OCA], [http://pdbe.org/1yye PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1yye RCSB], [http://www.ebi.ac.uk/pdbsum/1yye PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=1yye ProSAT]</span></td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=1yye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yye OCA], [http://pdbe.org/1yye PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1yye RCSB], [http://www.ebi.ac.uk/pdbsum/1yye PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=1yye ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 32:		Line 32:

	==See Also==		==See Also==
-	*[[Estrogen receptor\|Estrogen receptor]]	+	*[[Estrogen receptor 3D structures\|Estrogen receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 38:		Line 38:
	</StructureSection>		</StructureSection>
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Edsall, R J]]		[[Category: Edsall, R J]]
	[[Category: Harris, H A]]		[[Category: Harris, H A]]

OCA at 06:47, 25 April 2018

2018-04-25T06:47:41Z

←Older revision		Revision as of 06:47, 25 April 2018
Line 1:		Line 1:
		+
	==Crystal structure of estrogen receptor beta complexed with way-202196==		==Crystal structure of estrogen receptor beta complexed with way-202196==
	<StructureSection load='1yye' size='340' side='right' caption='[[1yye]], [[Resolution\|resolution]] 2.03Å' scene=''>		<StructureSection load='1yye' size='340' side='right' caption='[[1yye]], [[Resolution\|resolution]] 2.03Å' scene=''>
Line 6:		Line 7:
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1yy4\|1yy4]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1yy4\|1yy4]]</td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ESR2, ESTRB, NR3A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ESR2, ESTRB, NR3A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yye OCA], [http://pdbe.org/1yye PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1yye RCSB], [http://www.ebi.ac.uk/pdbsum/1yye PDBsum]</span></td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yye OCA], [http://pdbe.org/1yye PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1yye RCSB], [http://www.ebi.ac.uk/pdbsum/1yye PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=1yye ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 14:		Line 15:
	Check<jmol>		Check<jmol>
	<jmolCheckbox>		<jmolCheckbox>
-	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/yy/1yye_consurf.spt"</scriptWhenChecked>	+	<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/yy/1yye_consurf.spt"</scriptWhenChecked>
	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>		<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>

OCA at 06:20, 9 February 2016

2016-02-09T06:20:06Z

←Older revision		Revision as of 06:20, 9 February 2016
Line 18:		Line 18:
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>
	</jmolCheckbox>		</jmolCheckbox>
-	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/~~chain_selection~~.php?pdb_ID=~~2ata~~ ConSurf].	+	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1yye ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">

OCA at 19:26, 10 September 2015

2015-09-10T19:26:51Z

←Older revision		Revision as of 19:26, 10 September 2015
Line 2:		Line 2:
	<StructureSection load='1yye' size='340' side='right' caption='[[1yye]], [[Resolution\|resolution]] 2.03Å' scene=''>		<StructureSection load='1yye' size='340' side='right' caption='[[1yye]], [[Resolution\|resolution]] 2.03Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[1yye]] is a 4 chain structure with 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=1YYE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1YYE FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[1yye]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1YYE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1YYE FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=196:3-(3-FLUORO-4-HYDROXYPHENYL)-7-HYDROXY-1-NAPHTHONITRILE'>196</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=196:3-(3-FLUORO-4-HYDROXYPHENYL)-7-HYDROXY-1-NAPHTHONITRILE'>196</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1yy4\|1yy4]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1yy4\|1yy4]]</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ESR2, ESTRB, NR3A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 ~~Homo sapiens~~])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ESR2, ESTRB, NR3A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yye OCA], [http://www.rcsb.org/pdb/explore.do?structureId=1yye RCSB], [http://www.ebi.ac.uk/pdbsum/1yye PDBsum]</span></td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yye OCA], [http://pdbe.org/1yye PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1yye RCSB], [http://www.ebi.ac.uk/pdbsum/1yye PDBsum]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 28:		Line 28:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
		+	<div class="pdbe-citations 1yye" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 35:		Line 36:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Edsall, R J]]		[[Category: Edsall, R J]]
	[[Category: Harris, H A]]		[[Category: Harris, H A]]

OCA at 04:59, 25 December 2014

2014-12-25T04:59:08Z

←Older revision		Revision as of 04:59, 25 December 2014
Line 1:		Line 1:
-	~~{{STRUCTURE_1yye\| PDB=1yye \| SCENE= }}~~	+	==Crystal structure of estrogen receptor beta complexed with way-202196==
-	===Crystal structure of estrogen receptor beta complexed with way-202196===	+	<StructureSection load='1yye' size='340' side='right' caption='[[1yye]], [[Resolution\|resolution]] 2.03Å' scene=''>
-	~~{{ABSTRACT_PUBMED_15943471}}~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[1yye]] is a 4 chain structure with 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=1YYE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1YYE FirstGlance]. <br>
-	==Function==	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=196:3-(3-FLUORO-4-HYDROXYPHENYL)-7-HYDROXY-1-NAPHTHONITRILE'>196</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1yy4\|1yy4]]</td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ESR2, ESTRB, NR3A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
		+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yye OCA], [http://www.rcsb.org/pdb/explore.do?structureId=1yye RCSB], [http://www.ebi.ac.uk/pdbsum/1yye PDBsum]</span></td></tr>
		+	</table>
		+	== Function ==
	[[http://www.uniprot.org/uniprot/ESR2_HUMAN ESR2_HUMAN]] Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.		[[http://www.uniprot.org/uniprot/ESR2_HUMAN ESR2_HUMAN]] Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.
		+	== Evolutionary Conservation ==
		+	[[Image:Consurf_key_small.gif\|200px\|right]]
		+	Check<jmol>
		+	<jmolCheckbox>
		+	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/yy/1yye_consurf.spt"</scriptWhenChecked>
		+	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
		+	<text>to colour the structure by Evolutionary Conservation</text>
		+	</jmolCheckbox>
		+	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/chain_selection.php?pdb_ID=2ata ConSurf].
		+	<div style="clear:both"></div>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The 2-phenylnaphthalene scaffold was explored as a simplified version of genistein in order to identify ER selective ligands. With the aid of docking studies, positions 1, 4, and 8 of the 2-phenylnaphthalene template were predicted to be the most potentially influential positions to enhance ER selectivity using two different binding orientations. Both orientations have the phenol moiety mimicking the A-ring of genistein. Several compounds predicted to adopt orientations similar to that of genistein when bound to ERbeta were observed to have slightly higher ER affinity and selectivity than genistein. The second orientation we exploited, which was different from that of genistein when bound to ERbeta, resulted in the discovery of several compounds that had superior ER selectivity and affinity versus genistein. X-ray structures of two ER selective compounds (i.e., 15 and 47) confirmed the alternate binding mode and suggested that substituents at positions 1 and 8 were responsible for inducing selectivity. One compound (i.e., 47, WAY-202196) was further examined and found to be effective in two models of inflammation, suggesting that targeting ER may be therapeutically useful in treating certain chronic inflammatory diseases.

-	~~==About this Structure==~~	+	ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.,Mewshaw RE, Edsall RJ Jr, Yang C, Manas ES, Xu ZB, Henderson RA, Keith JC Jr, Harris HA J Med Chem. 2005 Jun 16;48(12):3953-79. PMID:15943471<ref>PMID:15943471</ref>
-	~~[[1yye]] is a 4 chain structure with 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=1YYE OCA].~~	+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>

	==See Also==		==See Also==
	*[[Estrogen receptor\|Estrogen receptor]]		*[[Estrogen receptor\|Estrogen receptor]]
-		+	== References ==
-	==~~Reference~~==	+	<references/>
-	~~<ref group="xtra">PMID:015943471</ref>~~<references ~~group="xtra"~~/><~~references~~/>	+	__TOC__
		+	</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
-	[[Category: Edsall, R J.]]	+	[[Category: Edsall, R J]]
-	[[Category: Harris, H A.]]	+	[[Category: Harris, H A]]
-	[[Category: Henderson, R A.]]	+	[[Category: Henderson, R A]]
-	[[Category: Keith, J C.]]	+	[[Category: Keith, J C]]
-	[[Category: Manas, E S.]]	+	[[Category: Manas, E S]]
-	[[Category: Mewshaw, R E.]]	+	[[Category: Mewshaw, R E]]
-	[[Category: Xu, Z B.]]	+	[[Category: Xu, Z B]]
-	[[Category: Yang, C.]]	+	[[Category: Yang, C]]
	[[Category: Agonist]]		[[Category: Agonist]]
	[[Category: Er]]		[[Category: Er]]

OCA at 03:42, 25 March 2013

2013-03-25T03:42:47Z

←Older revision		Revision as of 03:42, 25 March 2013
Line 1:		Line 1:
-	[[Image:1yye.png\|left\|200px]]
-
	{{STRUCTURE_1yye\| PDB=1yye \| SCENE= }}		{{STRUCTURE_1yye\| PDB=1yye \| SCENE= }}
-
	===Crystal structure of estrogen receptor beta complexed with way-202196===		===Crystal structure of estrogen receptor beta complexed with way-202196===
		+	{{ABSTRACT_PUBMED_15943471}}

-	~~{{ABSTRACT_PUBMED_15943471}}~~	+	==Function==
		+	[[http://www.uniprot.org/uniprot/ESR2_HUMAN ESR2_HUMAN]] Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.

	==About this Structure==		==About this Structure==
Line 14:		Line 13:

	==Reference==		==Reference==
-	<ref group="xtra">PMID:015943471</ref><references group="xtra"/>	+	<ref group="xtra">PMID:015943471</ref><references group="xtra"/><references/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Edsall, R J.]]		[[Category: Edsall, R J.]]

OCA at 12:56, 20 October 2012

2012-10-20T12:56:19Z

←Older revision		Revision as of 12:56, 20 October 2012
Line 8:		Line 8:

	==About this Structure==		==About this Structure==
-	[[1yye]] is a 4 chain structure ~~of [[Estrogen receptor]]~~ with 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=1YYE OCA].	+	[[1yye]] is a 4 chain structure with 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=1YYE OCA].

	==See Also==		==See Also==

OCA: Protected "1yye" [edit=sysop:move=sysop]

2012-07-26T10:24:00Z

Protected "1yye" [edit=sysop:move=sysop]

←Older revision

Revision as of 10:24, 26 July 2012

OCA at 10:23, 26 July 2012

2012-07-26T10:23:59Z

←Older revision		Revision as of 10:23, 26 July 2012
Line 1:		Line 1:
-	{{Seed}}
	[[Image:1yye.png\|left\|200px]]		[[Image:1yye.png\|left\|200px]]

-	<!--
-	The line below this paragraph, containing "STRUCTURE_1yye", creates the "Structure Box" on the page.
-	You may change the PDB parameter (which sets the PDB file loaded into the applet)
-	or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-	or leave the SCENE parameter empty for the default display.
-	-->
	{{STRUCTURE_1yye\| PDB=1yye \| SCENE= }}		{{STRUCTURE_1yye\| PDB=1yye \| SCENE= }}

	===Crystal structure of estrogen receptor beta complexed with way-202196===		===Crystal structure of estrogen receptor beta complexed with way-202196===

-
-	<!--
-	The line below this paragraph, {{ABSTRACT_PUBMED_15943471}}, adds the Publication Abstract to the page
-	(as it appears on PubMed at http://www.pubmed.gov), where 15943471 is the PubMed ID number.
-	-->
	{{ABSTRACT_PUBMED_15943471}}		{{ABSTRACT_PUBMED_15943471}}

	==About this Structure==		==About this Structure==
-	~~1YYE~~ is a 4 ~~chains~~ structure of ~~sequences~~ 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=1YYE OCA].	+	[[1yye]] is a 4 chain structure of [[Estrogen receptor]] with 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=1YYE OCA].
		+
		+	==See Also==
		+	*[[Estrogen receptor\|Estrogen receptor]]

	==Reference==		==Reference==
-	<ref group="xtra">PMID:~~15943471~~</ref><references group="xtra"/>	+	<ref group="xtra">PMID:015943471</ref><references group="xtra"/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
		+	[[Category: Edsall, R J.]]
	[[Category: Harris, H A.]]		[[Category: Harris, H A.]]
	[[Category: Henderson, R A.]]		[[Category: Henderson, R A.]]
-	[[Category: ~~Jr.~~, J C~~.Keith.]]~~	+	[[Category: Keith, J C.]]
-	~~[[Category: Jr., R J.Edsall~~.]]	+
	[[Category: Manas, E S.]]		[[Category: Manas, E S.]]
	[[Category: Mewshaw, R E.]]		[[Category: Mewshaw, R E.]]
Line 40:		Line 31:
	[[Category: Estrogen receptor beta]]		[[Category: Estrogen receptor beta]]
	[[Category: Nuclear receptor]]		[[Category: Nuclear receptor]]
		+	[[Category: Transcription]]
	[[Category: Transcription factor]]		[[Category: Transcription factor]]
-
-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Feb 17 07:10:32 2009''