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5eit
From Proteopedia
(Difference between revisions)
(New page: '''Unreleased structure''' The entry 5eit is ON HOLD until Paper Publication Authors: Nwachukwu, J.C., Srinivasan, S., Zheng, Y., Wang, S., Min, J., Dong, C., Liao, Z., Cavett, V., Nowa...) |
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal Structure of the ER-alpha Ligand-binding Domain (Y537S) in Complex with the imidazopyridine derivative 2-(4-hydroxyphenyl)-3-(trifluoromethyl)imidazo[1,2-a]pyridin-6-ol== | |
| + | <StructureSection load='5eit' size='340' side='right'caption='[[5eit]], [[Resolution|resolution]] 2.68Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5eit]] 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=5EIT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5EIT FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.68Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=5P1:2-(4-HYDROXYPHENYL)-3-(TRIFLUOROMETHYL)IMIDAZO[1,2-A]PYRIDIN-6-OL'>5P1</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=5eit FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eit OCA], [https://pdbe.org/5eit PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5eit RCSB], [https://www.ebi.ac.uk/pdbsum/5eit PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5eit ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == 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> | ||
| - | + | ==See Also== | |
| - | + | *[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]] | |
| - | + | == References == | |
| - | [[Category: | + | <references/> |
| - | [[Category: | + | __TOC__ |
| - | [[Category: | + | </StructureSection> |
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: | + | [[Category: Carlson KE]] |
| - | [[Category: | + | [[Category: Cavett V]] |
| - | [[Category: | + | [[Category: Dong C]] |
| - | [[Category: | + | [[Category: Elemento O]] |
| - | [[Category: | + | [[Category: Houtman R]] |
| - | [[Category: | + | [[Category: Josan JS]] |
| - | [[Category: | + | [[Category: Katzenellenbogen JA]] |
| - | [[Category: Nowak | + | [[Category: Liao Z]] |
| - | [[Category: | + | [[Category: Min J]] |
| - | [[Category: | + | [[Category: Nettles KW]] |
| - | [[Category: | + | [[Category: Nowak J]] |
| - | [[Category: | + | [[Category: Nwachukwu JC]] |
| + | [[Category: Srinivasan S]] | ||
| + | [[Category: Wang S]] | ||
| + | [[Category: Zheng Y]] | ||
| + | [[Category: Zhou HB]] | ||
Current revision
Crystal Structure of the ER-alpha Ligand-binding Domain (Y537S) in Complex with the imidazopyridine derivative 2-(4-hydroxyphenyl)-3-(trifluoromethyl)imidazo[1,2-a]pyridin-6-ol
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Categories: Homo sapiens | Large Structures | Carlson KE | Cavett V | Dong C | Elemento O | Houtman R | Josan JS | Katzenellenbogen JA | Liao Z | Min J | Nettles KW | Nowak J | Nwachukwu JC | Srinivasan S | Wang S | Zheng Y | Zhou HB
