2yat

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[[Image:2yat.png|left|200px]]
 
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{{STRUCTURE_2yat| PDB=2yat | SCENE= }}
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==Crystal structure of estradiol derived metal chelate and estrogen receptor-ligand binding domain complex==
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<StructureSection load='2yat' size='340' side='right'caption='[[2yat]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2yat]] 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=2YAT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2YAT FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.602&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EEU:ESTRADIOL-PYRIDINIUM+TETRAACETIC+ACID'>EEU</scene>, <scene name='pdbligand=EU:EUROPIUM+ION'>EU</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2yat FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2yat OCA], [https://pdbe.org/2yat PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2yat RCSB], [https://www.ebi.ac.uk/pdbsum/2yat PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2yat ProSAT]</span></td></tr>
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</table>
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== Function ==
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[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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Selective estrogen receptor modulators, such as estradiol 17alpha-derived metal complexes, have been synthesized as targeted probes for the diagnosis and treatment of breast cancer. Here, we report the detailed 3D structure of estrogen receptor alpha ligand-binding domain (ERalpha-LBD) bound with a novel estradiol-derived metal complex, estradiol-pyridine tetra acetate europium (III) at 2.6A resolution. This structure provides important information pertinent to the design of novel functional ERalpha targeted probes for clinical applications.
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===Crystal structure of estradiol derived metal chelate and estrogen receptor-ligand binding domain complex===
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Structure of estradiol metal chelate and estrogen receptor complex: The basis for designing a new class of selective estrogen receptor modulators.,Li MJ, Greenblatt HM, Dym O, Albeck S, Pais A, Gunanathan C, Milstein D, Degani H, Sussman JL J Med Chem. 2011 Apr 7. PMID:21473635<ref>PMID:21473635</ref>
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{{ABSTRACT_PUBMED_21473635}}
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==About this Structure==
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<div class="pdbe-citations 2yat" style="background-color:#fffaf0;"></div>
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[[2yat]] is a 1 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=2YAT OCA].
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==See Also==
==See Also==
*[[Estrogen receptor|Estrogen receptor]]
*[[Estrogen receptor|Estrogen receptor]]
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*[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]]
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==Reference==
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== References ==
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<ref group="xtra">PMID:021473635</ref><references group="xtra"/>
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<references/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Albeck, S.]]
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[[Category: Large Structures]]
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[[Category: Degani, H.]]
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[[Category: Albeck S]]
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[[Category: Dym, O.]]
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[[Category: Degani H]]
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[[Category: Greenblatt, H M.]]
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[[Category: Dym O]]
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[[Category: Li, M J.]]
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[[Category: Greenblatt HM]]
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[[Category: Sussman, J L.]]
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[[Category: Li MJ]]
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[[Category: Transcription]]
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[[Category: Sussman JL]]

Current revision

Crystal structure of estradiol derived metal chelate and estrogen receptor-ligand binding domain complex

PDB ID 2yat

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