8dud - Revision history

OCA at 10:14, 25 October 2023

OCA — Wed, 25 Oct 2023 10:14:34 GMT

←Older revision		Revision as of 10:14, 25 October 2023
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[8dud]] is a 1 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=8DUD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8DUD FirstGlance]. <br>		<table><tr><td colspan='2'>[[8dud]] is a 1 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=8DUD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8DUD FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=TV3:[(1R)-6-hydroxy-1-(4-{[(3R)-1-propylpyrrolidin-3-yl]methoxy}phenyl)-1,4-dihydro-2H-spiro[cyclopropane-1,3-isoquinolin]-2-yl](phenyl)methanone'>TV3</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]] 1.81Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=TV3:[(1R)-6-hydroxy-1-(4-{[(3R)-1-propylpyrrolidin-3-yl]methoxy}phenyl)-1,4-dihydro-2H-spiro[cyclopropane-1,3-isoquinolin]-2-yl](phenyl)methanone'>TV3</scene></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=8dud FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8dud OCA], [https://pdbe.org/8dud PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8dud RCSB], [https://www.ebi.ac.uk/pdbsum/8dud PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8dud ProSAT]</span></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=8dud FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8dud OCA], [https://pdbe.org/8dud PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8dud RCSB], [https://www.ebi.ac.uk/pdbsum/8dud PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8dud ProSAT]</span></td></tr>
	</table>		</table>

OCA at 04:16, 25 May 2023

OCA — Thu, 25 May 2023 04:16:06 GMT

←Older revision		Revision as of 04:16, 25 May 2023
Line 9:		Line 9:
	== Function ==		== Function ==
	[https://www.uniprot.org/uniprot/ESR1_HUMAN ESR1_HUMAN] Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full length receptor. Isoform 3 can bind to ERE and inhibit isoform 1.<ref>PMID:7651415</ref> <ref>PMID:10970861</ref> <ref>PMID:9328340</ref> <ref>PMID:10681512</ref> <ref>PMID:10816575</ref> <ref>PMID:11477071</ref> <ref>PMID:11682626</ref> <ref>PMID:15078875</ref> <ref>PMID:16043358</ref> <ref>PMID:15891768</ref> <ref>PMID:16684779</ref> <ref>PMID:18247370</ref> <ref>PMID:17932106</ref> <ref>PMID:19350539</ref> <ref>PMID:20705611</ref> <ref>PMID:21937726</ref> <ref>PMID:21330404</ref> <ref>PMID:22083956</ref>		[https://www.uniprot.org/uniprot/ESR1_HUMAN ESR1_HUMAN] Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full length receptor. Isoform 3 can bind to ERE and inhibit isoform 1.<ref>PMID:7651415</ref> <ref>PMID:10970861</ref> <ref>PMID:9328340</ref> <ref>PMID:10681512</ref> <ref>PMID:10816575</ref> <ref>PMID:11477071</ref> <ref>PMID:11682626</ref> <ref>PMID:15078875</ref> <ref>PMID:16043358</ref> <ref>PMID:15891768</ref> <ref>PMID:16684779</ref> <ref>PMID:18247370</ref> <ref>PMID:17932106</ref> <ref>PMID:19350539</ref> <ref>PMID:20705611</ref> <ref>PMID:21937726</ref> <ref>PMID:21330404</ref> <ref>PMID:22083956</ref>
		+
		+	==See Also==
		+	*[[Estrogen receptor 3D structures\|Estrogen receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 07:34, 9 November 2022

OCA — Wed, 09 Nov 2022 07:34:51 GMT

←Older revision		Revision as of 07:34, 9 November 2022
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry 8dud is ON HOLD until Paper Publication~~	+	==Estrogen Receptor Alpha Ligand Binding Domain in Complex with (6'-hydroxy-1'-(4-(2-(1-propylpyrrolidin-3-yl)ethoxy)phenyl)-1',4'-dihydro-2'<i>H</i>-spiro[cyclopropane-1,3'-isoquinolin]-2'-yl)(phenyl)methanone==
-		+	<StructureSection load='8dud' size='340' side='right'caption='[[8dud]], [[Resolution\|resolution]] 1.81Å' scene=''>
-	~~Authors: Hancock, G.R., Young, K.S., Hosfield, D.J., Joiner, C., Sullivan, E.A., Yildz, Y., Laine, M., Greene, G.L., Fanning, S.W.~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[8dud]] is a 1 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=8DUD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8DUD FirstGlance]. <br>
-	~~Description:~~ Estrogen Receptor Alpha Ligand Binding Domain in Complex with (6''-hydroxy-1''-(4-(2-(1-propylpyrrolidin-3-yl)ethoxy)phenyl)-1'',4''-dihydro-2''<i>H</i>-spiro[cyclopropane-1,3''-isoquinolin]-2''-yl)(phenyl)methanone	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=TV3:[(1R)-6-hydroxy-1-(4-{[(3R)-1-propylpyrrolidin-3-yl]methoxy}phenyl)-1,4-dihydro-2H-spiro[cyclopropane-1,3-isoquinolin]-2-yl](phenyl)methanone'>TV3</scene></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8dud FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8dud OCA], [https://pdbe.org/8dud PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8dud RCSB], [https://www.ebi.ac.uk/pdbsum/8dud PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8dud ProSAT]</span></td></tr>
-	[[Category: ~~Young, K.S~~]]	+	</table>
-	[[Category: ~~Joiner, C~~]]	+	== Function ==
-	[[Category: ~~Hosfield, D.J~~]]	+	[https://www.uniprot.org/uniprot/ESR1_HUMAN ESR1_HUMAN] Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full length receptor. Isoform 3 can bind to ERE and inhibit isoform 1.<ref>PMID:7651415</ref> <ref>PMID:10970861</ref> <ref>PMID:9328340</ref> <ref>PMID:10681512</ref> <ref>PMID:10816575</ref> <ref>PMID:11477071</ref> <ref>PMID:11682626</ref> <ref>PMID:15078875</ref> <ref>PMID:16043358</ref> <ref>PMID:15891768</ref> <ref>PMID:16684779</ref> <ref>PMID:18247370</ref> <ref>PMID:17932106</ref> <ref>PMID:19350539</ref> <ref>PMID:20705611</ref> <ref>PMID:21937726</ref> <ref>PMID:21330404</ref> <ref>PMID:22083956</ref>
-	[[Category: Hancock~~, G.R~~]]	+	== References ==
-	[[Category: ~~Greene, G.L~~]]	+	<references/>
-	[[Category: ~~Fanning, S.W~~]]	+	__TOC__
-	[[Category: Laine, M]]	+	</StructureSection>
-	[[Category: Sullivan~~, E.A~~]]	+	[[Category: Homo sapiens]]
-	[[Category: Yildz, Y]]	+	[[Category: Large Structures]]
		+	[[Category: Fanning SW]]
		+	[[Category: Greene GL]]
		+	[[Category: Hancock GR]]
		+	[[Category: Hosfield DJ]]
		+	[[Category: Joiner C]]
		+	[[Category: Laine M]]
		+	[[Category: Sullivan EA]]
		+	[[Category: Yildz Y]]
		+	[[Category: Young KS]]

OCA at 05:32, 31 August 2022

OCA — Wed, 31 Aug 2022 05:32:25 GMT

←Older revision		Revision as of 05:32, 31 August 2022
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 8dud is ON HOLD	+	The entry 8dud is ON HOLD until Paper Publication

	Authors: Hancock, G.R., Young, K.S., Hosfield, D.J., Joiner, C., Sullivan, E.A., Yildz, Y., Laine, M., Greene, G.L., Fanning, S.W.		Authors: Hancock, G.R., Young, K.S., Hosfield, D.J., Joiner, C., Sullivan, E.A., Yildz, Y., Laine, M., Greene, G.L., Fanning, S.W.
Line 7:		Line 7:
	Description: Estrogen Receptor Alpha Ligand Binding Domain in Complex with (6''-hydroxy-1''-(4-(2-(1-propylpyrrolidin-3-yl)ethoxy)phenyl)-1'',4''-dihydro-2''<i>H</i>-spiro[cyclopropane-1,3''-isoquinolin]-2''-yl)(phenyl)methanone		Description: Estrogen Receptor Alpha Ligand Binding Domain in Complex with (6''-hydroxy-1''-(4-(2-(1-propylpyrrolidin-3-yl)ethoxy)phenyl)-1'',4''-dihydro-2''<i>H</i>-spiro[cyclopropane-1,3''-isoquinolin]-2''-yl)(phenyl)methanone
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
-	[[Category: Laine, M]]
-	[[Category: Sullivan, E.A]]
	[[Category: Young, K.S]]		[[Category: Young, K.S]]
	[[Category: Joiner, C]]		[[Category: Joiner, C]]
Line 15:		Line 13:
	[[Category: Greene, G.L]]		[[Category: Greene, G.L]]
	[[Category: Fanning, S.W]]		[[Category: Fanning, S.W]]
		+	[[Category: Laine, M]]
		+	[[Category: Sullivan, E.A]]
	[[Category: Yildz, Y]]		[[Category: Yildz, Y]]

OCA: Protected "8dud" [edit=sysop:move=sysop]

OCA — Wed, 03 Aug 2022 03:58:05 GMT

Protected "8dud" [edit=sysop:move=sysop]

←Older revision

Revision as of 03:58, 3 August 2022

OCA: New page: '''Unreleased structure''' The entry 8dud is ON HOLD Authors: Hancock, G.R., Young, K.S., Hosfield, D.J., Joiner, C., Sullivan, E.A., Yildz, Y., Laine, M., Greene, G.L., Fanning, S.W. ...

OCA — Wed, 03 Aug 2022 03:58:04 GMT

New page: '''Unreleased structure''' The entry 8dud is ON HOLD Authors: Hancock, G.R., Young, K.S., Hosfield, D.J., Joiner, C., Sullivan, E.A., Yildz, Y., Laine, M., Greene, G.L., Fanning, S.W. ...

New page

'''Unreleased structure'''

The entry 8dud is ON HOLD

Authors: Hancock, G.R., Young, K.S., Hosfield, D.J., Joiner, C., Sullivan, E.A., Yildz, Y., Laine, M., Greene, G.L., Fanning, S.W.

Description: Estrogen Receptor Alpha Ligand Binding Domain in Complex with (6''-hydroxy-1''-(4-(2-(1-propylpyrrolidin-3-yl)ethoxy)phenyl)-1'',4''-dihydro-2''<i>H</i>-spiro[cyclopropane-1,3''-isoquinolin]-2''-yl)(phenyl)methanone
[[Category: Unreleased Structures]]
[[Category: Laine, M]]
[[Category: Sullivan, E.A]]
[[Category: Young, K.S]]
[[Category: Joiner, C]]
[[Category: Hosfield, D.J]]
[[Category: Hancock, G.R]]
[[Category: Greene, G.L]]
[[Category: Fanning, S.W]]
[[Category: Yildz, Y]]