6vpk - Revision history

OCA: Redirecting to 7ujy

OCA — Wed, 15 Jun 2022 05:07:13 GMT

Redirecting to 7ujy

←Older revision		Revision as of 05:07, 15 June 2022
Line 1:		Line 1:
-		+	#REDIRECT [[7ujy]] This PDB entry is obsolete and replaced by 7ujy
-	~~==Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with a Methylated Lasofoxifene Derivative that Enhances Estrogen Receptor Alpha Nuclear Resonance Time==~~	+
-	~~<StructureSection load='6vpk' size='340' side='right'caption='~~[[~~6vpk]], [[Resolution\|resolution]] 1.70Å' scene=''>~~	+
-	~~== Structural highlights ==~~	+
-	~~<table><tr><td colspan='2'>[[6vpk~~]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6VPK OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6VPK FirstGlance]. <br>	+
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=RL4:(5R,6S)-5-(4-{2-[(2R)-2-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol'>RL4</scene></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=6vpk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6vpk OCA], [http://pdbe.org/6vpk PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6vpk RCSB], [http://www.ebi.ac.uk/pdbsum/6vpk PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6vpk ProSAT]</span></td></tr>	+
-	~~</table>~~	+
-	~~== Function ==~~	+
-	~~[[http://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>	+
-	~~== References ==~~	+
-	~~<references/>~~	+
-	~~__TOC__~~	+
-	~~</StructureSection>~~	+
-	~~[[Category: Large Structures]]~~	+
-	~~[[Category: Fanning, S W]]~~	+
-	~~[[Category: Greene, G L]]~~	+
-	~~[[Category: Alpha helical bundle]]~~	+
-	~~[[Category: Antiestrogen]]~~	+
-	~~[[Category: Breast cancer]]~~	+
-	~~[[Category: Drug resistance]]~~	+
-	~~[[Category: Estrogen receptor alpha]]~~	+
-	~~[[Category: Serm]]~~	+
-	~~[[Category: Transcription]]~~	+

OCA at 10:01, 18 March 2020

OCA — Wed, 18 Mar 2020 10:01:20 GMT

←Older revision		Revision as of 10:01, 18 March 2020
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry 6vpk is ON HOLD~~	+	==Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with a Methylated Lasofoxifene Derivative that Enhances Estrogen Receptor Alpha Nuclear Resonance Time==
-		+	<StructureSection load='6vpk' size='340' side='right'caption='[[6vpk]], [[Resolution\|resolution]] 1.70Å' scene=''>
-	~~Authors: Fanning, S.W., Greene, G.L.~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[6vpk]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6VPK OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6VPK FirstGlance]. <br>
-	~~Description:~~ Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with a Methylated Lasofoxifene Derivative that Enhances Estrogen Receptor Alpha Nuclear Resonance Time	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=RL4:(5R,6S)-5-(4-{2-[(2R)-2-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol'>RL4</scene></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	<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=6vpk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6vpk OCA], [http://pdbe.org/6vpk PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6vpk RCSB], [http://www.ebi.ac.uk/pdbsum/6vpk PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6vpk ProSAT]</span></td></tr>
-	[[Category: Greene, G.L]]	+	</table>
-	[[Category: ~~Fanning, S.W~~]]	+	== Function ==
		+	[[http://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>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Fanning, S W]]
		+	[[Category: Greene, G L]]
		+	[[Category: Alpha helical bundle]]
		+	[[Category: Antiestrogen]]
		+	[[Category: Breast cancer]]
		+	[[Category: Drug resistance]]
		+	[[Category: Estrogen receptor alpha]]
		+	[[Category: Serm]]
		+	[[Category: Transcription]]

OCA: Protected "6vpk" [edit=sysop:move=sysop]

OCA — Thu, 13 Feb 2020 02:44:48 GMT

Protected "6vpk" [edit=sysop:move=sysop]

←Older revision

Revision as of 02:44, 13 February 2020

OCA: New page: '''Unreleased structure''' The entry 6vpk is ON HOLD Authors: Fanning, S.W., Greene, G.L. Description: Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with a Meth...

OCA — Thu, 13 Feb 2020 02:44:46 GMT

New page: '''Unreleased structure''' The entry 6vpk is ON HOLD Authors: Fanning, S.W., Greene, G.L. Description: Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with a Meth...

New page

'''Unreleased structure'''

The entry 6vpk is ON HOLD

Authors: Fanning, S.W., Greene, G.L.

Description: Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with a Methylated Lasofoxifene Derivative that Enhances Estrogen Receptor Alpha Nuclear Resonance Time
[[Category: Unreleased Structures]]
[[Category: Greene, G.L]]
[[Category: Fanning, S.W]]