6dfn - Revision history

OCA at 14:33, 13 March 2024

2024-03-13T14:33:59Z

←Older revision		Revision as of 14:33, 13 March 2024
Line 1:		Line 1:

	==Crystal structure of estrogen receptor alpha in complex with receptor degrader 16aa==		==Crystal structure of estrogen receptor alpha in complex with receptor degrader 16aa==
-	<StructureSection load='6dfn' size='340' side='right' caption='[[6dfn]], [[Resolution\|resolution]] 2.10Å' scene=''>	+	<StructureSection load='6dfn' size='340' side='right'caption='[[6dfn]], [[Resolution\|resolution]] 2.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6dfn]] 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=6DFN OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6DFN FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6dfn]] 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=6DFN OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6DFN FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=G91:(8S)-8-(4-{2-[3-(fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-1,8-dihydro-2H-[1]benzopyrano[4,3-d][1]benzoxepine-5,11-diol'>G91</scene>, <scene name='pdbligand=G9J:(2S)-3-(3-hydroxyphenyl)-2-(4-iodophenyl)-4-methyl-2H-1-benzopyran-6-ol'>G9J</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</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]] 2.1Å</td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ESR1, ESR, NR3A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])~~</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=G91:(8S)-8-(4-{2-[3-(fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-1,8-dihydro-2H-[1]benzopyrano[4,3-d][1]benzoxepine-5,11-diol'>G91</scene>, <scene name='pdbligand=G9J:(2S)-3-(3-hydroxyphenyl)-2-(4-iodophenyl)-4-methyl-2H-1-benzopyran-6-ol'>G9J</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</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=6dfn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dfn OCA], [~~http~~://pdbe.org/6dfn PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6dfn RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6dfn PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6dfn 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=6dfn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dfn OCA], [https://pdbe.org/6dfn PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6dfn RCSB], [https://www.ebi.ac.uk/pdbsum/6dfn PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6dfn ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== 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>	+	[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>
-	~~<div style="background-color:#fffaf0;">~~	+
-	~~== Publication Abstract from PubMed ==~~	+
-	Despite tremendous progress made in the understanding of the ERalpha signaling pathway and the approval of many therapeutic agents, ER+breast cancer continues to be a leading cause of cancer death in women. We set out to discover compounds with a dual mechanism of action in which they not only compete with estradiol for binding with ERalpha, but also can induce the degradation of the ERalpha protein itself. We were attracted to the constrained chromenes containing a tetracyclic benzopyranobenzoxepine scaffold, which were reported as potent selective estrogen receptor modulators (SERMs). Incorporation of a fluoromethyl azetidine side chain yielded highly potent and efficacious selective estrogen receptor degraders (SERDs), such as 16aa and surprisingly, also its enantiomeric pair 16ab. Co-crystal structures of the enantiomeric pair 16aa and 16ab in complex with ERalpha revealed default (mimics the A-D rings of endogenous ligand estradiol) and core-flipped binding modes, rationalizing the equivalent potency observed for these enantiomers in the ERalpha degradation and MCF-7 anti-proliferation assays.	+

-	Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.,Zhang B, Kiefer JR, Blake RA, Chang JH, Hartman S, Ingalla ER, Kleinheinz T, Mody V, Nannini M, Ortwine DF, Ran Y, Sambrone A, Sampath D, Vinogradova M, Zhong Y, Nwachukwu JC, Nettles KW, Lai T, Liao J, Zheng X, Chen H, Wang X, Liang J Bioorg Med Chem Lett. 2019 Feb 1. pii: S0960-894X(19)30057-5. doi:, 10.1016/j.bmcl.2019.01.036. PMID:30732944<ref>PMID:30732944</ref>	+	==See Also==
-		+	*[[Estrogen receptor 3D structures\|Estrogen receptor 3D structures]]
-	~~From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~	+
-	~~</div>~~	+
-	~~<div class~~=~~"pdbe-citations 6dfn" style~~=~~"background-color:#fffaf0;"></div>~~	+
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
-	[[Category: Kiefer~~, J R~~]]	+	[[Category: Large Structures]]
-	[[Category: Liang, J]]	+	[[Category: Kiefer JR]]
-	[[Category: Nettles~~, K W~~]]	+	[[Category: Liang J]]
-	[[Category: Nwachukwu~~, J C~~]]	+	[[Category: Nettles KW]]
-	[[Category: Ortwine~~, D F~~]]	+	[[Category: Nwachukwu JC]]
-	[[Category: Vinogradova, M]]	+	[[Category: Ortwine DF]]
-	[[Category: Zhang, B]]	+	[[Category: Vinogradova M]]
-	~~[[Category: Antagonist]]~~	+	[[Category: Zhang B]]
-	~~[[Category: Breast cancer]]~~	+
-	~~[[Category: Degrader]]~~	+
-	~~[[Category: Era]]~~	+
-	~~[[Category: Estrogen receptor]]~~	+
-	~~[[Category: Inverse agonist]]~~	+
-	~~[[Category: Ligand]]~~	+
-	~~[[Category: Nuclear protein]]~~	+
-	~~[[Category: Receptor~~]]	+

OCA at 08:19, 6 March 2019

2019-03-06T08:19:59Z

←Older revision		Revision as of 08:19, 6 March 2019
Line 1:		Line 1:

	==Crystal structure of estrogen receptor alpha in complex with receptor degrader 16aa==		==Crystal structure of estrogen receptor alpha in complex with receptor degrader 16aa==
-	<StructureSection load='6dfn' size='340' side='right' caption='[[6dfn]], [[Resolution\|resolution]] 2.10Å' scene=''>	+	<StructureSection load='6dfn' size='340' side='right' caption='[[6dfn]], [[Resolution\|resolution]] 2.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6dfn]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6DFN OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6DFN FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6dfn]] 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=6DFN OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6DFN FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=G91:(8S)-8-(4-{2-[3-(fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-1,8-dihydro-2H-[1]benzopyrano[4,3-d][1]benzoxepine-5,11-diol'>G91</scene>, <scene name='pdbligand=G9J:(2S)-3-(3-hydroxyphenyl)-2-(4-iodophenyl)-4-methyl-2H-1-benzopyran-6-ol'>G9J</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=G91:(8S)-8-(4-{2-[3-(fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-1,8-dihydro-2H-[1]benzopyrano[4,3-d][1]benzoxepine-5,11-diol'>G91</scene>, <scene name='pdbligand=G9J:(2S)-3-(3-hydroxyphenyl)-2-(4-iodophenyl)-4-methyl-2H-1-benzopyran-6-ol'>G9J</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ESR1, ESR, NR3A1 ([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=6dfn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dfn OCA], [http://pdbe.org/6dfn PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6dfn RCSB], [http://www.ebi.ac.uk/pdbsum/6dfn PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6dfn ProSAT]</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=6dfn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dfn OCA], [http://pdbe.org/6dfn PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6dfn RCSB], [http://www.ebi.ac.uk/pdbsum/6dfn PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6dfn ProSAT]</span></td></tr>
	</table>		</table>
Line 22:		Line 23:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Kiefer, J R]]		[[Category: Kiefer, J R]]
	[[Category: Liang, J]]		[[Category: Liang, J]]

OCA at 06:38, 21 February 2019

2019-02-21T06:38:09Z

←Older revision		Revision as of 06:38, 21 February 2019
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 6dfn is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==Crystal structure of estrogen receptor alpha in complex with receptor degrader 16aa==
		+	<StructureSection load='6dfn' size='340' side='right' caption='[[6dfn]], [[Resolution\|resolution]] 2.10Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[6dfn]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6DFN OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6DFN FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=G91:(8S)-8-(4-{2-[3-(fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-1,8-dihydro-2H-[1]benzopyrano[4,3-d][1]benzoxepine-5,11-diol'>G91</scene>, <scene name='pdbligand=G9J:(2S)-3-(3-hydroxyphenyl)-2-(4-iodophenyl)-4-methyl-2H-1-benzopyran-6-ol'>G9J</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</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=6dfn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dfn OCA], [http://pdbe.org/6dfn PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6dfn RCSB], [http://www.ebi.ac.uk/pdbsum/6dfn PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6dfn 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>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Despite tremendous progress made in the understanding of the ERalpha signaling pathway and the approval of many therapeutic agents, ER+breast cancer continues to be a leading cause of cancer death in women. We set out to discover compounds with a dual mechanism of action in which they not only compete with estradiol for binding with ERalpha, but also can induce the degradation of the ERalpha protein itself. We were attracted to the constrained chromenes containing a tetracyclic benzopyranobenzoxepine scaffold, which were reported as potent selective estrogen receptor modulators (SERMs). Incorporation of a fluoromethyl azetidine side chain yielded highly potent and efficacious selective estrogen receptor degraders (SERDs), such as 16aa and surprisingly, also its enantiomeric pair 16ab. Co-crystal structures of the enantiomeric pair 16aa and 16ab in complex with ERalpha revealed default (mimics the A-D rings of endogenous ligand estradiol) and core-flipped binding modes, rationalizing the equivalent potency observed for these enantiomers in the ERalpha degradation and MCF-7 anti-proliferation assays.

-	~~Authors:~~ Kiefer, ~~J.R.~~, ~~Vinogradova~~, M., ~~Liang~~, J., ~~Zhang~~, B., Ortwine, D~~.F.~~, ~~Nettles~~, ~~K.W.~~, Nwachukwu, J.C.	+	Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.,Zhang B, Kiefer JR, Blake RA, Chang JH, Hartman S, Ingalla ER, Kleinheinz T, Mody V, Nannini M, Ortwine DF, Ran Y, Sambrone A, Sampath D, Vinogradova M, Zhong Y, Nwachukwu JC, Nettles KW, Lai T, Liao J, Zheng X, Chen H, Wang X, Liang J Bioorg Med Chem Lett. 2019 Feb 1. pii: S0960-894X(19)30057-5. doi:, 10.1016/j.bmcl.2019.01.036. PMID:30732944<ref>PMID:30732944</ref>

-	~~Description: Crystal structure~~ of ~~estrogen receptor alpha in complex with receptor degrader 16aa~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[Category: Unreleased Structures]]~~	+	</div>
-	~~[[Category~~: ~~Zhang, B]]~~	+	<div class="pdbe-citations 6dfn" style="background-color:#fffaf0;"></div>
-	[[Category: Kiefer, J.R]]	+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Kiefer, J R]]
	[[Category: Liang, J]]		[[Category: Liang, J]]
-	[[Category: ~~Nwachukwu~~, ~~J.C~~]]	+	[[Category: Nettles, K W]]
-	[[Category: ~~Nettles~~, ~~K.W~~]]	+	[[Category: Nwachukwu, J C]]
-	[[Category: Ortwine, D.F]]	+	[[Category: Ortwine, D F]]
	[[Category: Vinogradova, M]]		[[Category: Vinogradova, M]]
		+	[[Category: Zhang, B]]
		+	[[Category: Antagonist]]
		+	[[Category: Breast cancer]]
		+	[[Category: Degrader]]
		+	[[Category: Era]]
		+	[[Category: Estrogen receptor]]
		+	[[Category: Inverse agonist]]
		+	[[Category: Ligand]]
		+	[[Category: Nuclear protein]]
		+	[[Category: Receptor]]

OCA at 06:08, 10 October 2018

2018-10-10T06:08:49Z

←Older revision		Revision as of 06:08, 10 October 2018
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6dfn is ON HOLD	+	The entry 6dfn is ON HOLD until Paper Publication

	Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Zhang, B., Ortwine, D.F., Nettles, K.W., Nwachukwu, J.C.		Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Zhang, B., Ortwine, D.F., Nettles, K.W., Nwachukwu, J.C.

OCA at 06:10, 3 October 2018

2018-10-03T06:10:24Z

←Older revision		Revision as of 06:10, 3 October 2018
Line 5:		Line 5:
	Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Zhang, B., Ortwine, D.F., Nettles, K.W., Nwachukwu, J.C.		Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Zhang, B., Ortwine, D.F., Nettles, K.W., Nwachukwu, J.C.

-	Description: Crystal structure of estrogen receptor alpha in complex with receptor degrader ~~16ab~~	+	Description: Crystal structure of estrogen receptor alpha in complex with receptor degrader 16aa
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
	[[Category: Zhang, B]]		[[Category: Zhang, B]]
-	[[Category: Nwachukwu, J.C]]
-	[[Category: Ortwine, D.F]]
	[[Category: Kiefer, J.R]]		[[Category: Kiefer, J.R]]
	[[Category: Liang, J]]		[[Category: Liang, J]]
		+	[[Category: Nwachukwu, J.C]]
	[[Category: Nettles, K.W]]		[[Category: Nettles, K.W]]
		+	[[Category: Ortwine, D.F]]
	[[Category: Vinogradova, M]]		[[Category: Vinogradova, M]]

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

2018-05-23T06:03:24Z

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

←Older revision

Revision as of 06:03, 23 May 2018

OCA: New page: '''Unreleased structure''' The entry 6dfn is ON HOLD Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Zhang, B., Ortwine, D.F., Nettles, K.W., Nwachukwu, J.C. Description: Crystal st...

2018-05-23T06:03:22Z

New page: '''Unreleased structure''' The entry 6dfn is ON HOLD Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Zhang, B., Ortwine, D.F., Nettles, K.W., Nwachukwu, J.C. Description: Crystal st...

New page

'''Unreleased structure'''

The entry 6dfn is ON HOLD

Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Zhang, B., Ortwine, D.F., Nettles, K.W., Nwachukwu, J.C.

Description: Crystal structure of estrogen receptor alpha in complex with receptor degrader 16ab
[[Category: Unreleased Structures]]
[[Category: Zhang, B]]
[[Category: Nwachukwu, J.C]]
[[Category: Ortwine, D.F]]
[[Category: Kiefer, J.R]]
[[Category: Liang, J]]
[[Category: Nettles, K.W]]
[[Category: Vinogradova, M]]