5die: Difference between revisions
New page: '''Unreleased structure''' The entry 5die is ON HOLD Authors: Nwachukwu, J.C., Srinivasan, S., Zheng, Y., Wang, S., Min, J., Dong, C., Liao, Z., Cavett, V., Nowak, J., Houtman, R., Carl... |
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The | ==Crystal Structure of the ER-alpha Ligand-binding Domain in complex with a trifluoro-substituted A-CD ring estrogen derivative (1S,3aR,5S,7aS)-7a-methyl-5-(2,3,5-trifluoro-4-hydroxyphenyl)octahydro-1H-inden-1-ol== | ||
<StructureSection load='5die' size='340' side='right'caption='[[5die]], [[Resolution|resolution]] 2.24Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[5die]] 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=5DIE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5DIE 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]] 2.24Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=5CJ:(1S,3AR,5S,7AS)-7A-METHYL-5-(2,3,5-TRIFLUORO-4-HYDROXYPHENYL)OCTAHYDRO-1H-INDEN-1-OL'>5CJ</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=5die FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5die OCA], [https://pdbe.org/5die PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5die RCSB], [https://www.ebi.ac.uk/pdbsum/5die PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5die 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: | [[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]] |