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5kce
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal Structure of the ER-alpha Ligand-binding Domain (Y537S) in Complex with an N-methyl, 2-chlorobenzyl OBHS-N derivative== | |
| - | + | <StructureSection load='5kce' size='340' side='right' caption='[[5kce]], [[Resolution|resolution]] 1.85Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[5kce]] is a 4 chain structure. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=4zwh 4zwh]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5KCE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5KCE FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=OB3:(1S,2R,4S)-N-(2-CHLOROPHENYL)-5,6-BIS(4-HYDROXYPHENYL)-N-METHYL-7-OXABICYCLO[2.2.1]HEPT-5-ENE-2-SULFONAMIDE'>OB3</scene></td></tr> | |
| - | [[Category: | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5kcc|5kcc]], [[5kcd|5kcd]], [[5kcf|5kcf]], [[5kct|5kct]], [[5kcu|5kcu]], [[5kcw|5kcw]], [[5kd9|5kd9]]</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=5kce FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kce OCA], [http://pdbe.org/5kce PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5kce RCSB], [http://www.ebi.ac.uk/pdbsum/5kce PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5kce ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Disease == | ||
| + | [[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Note=Chromosomal aberrations involving NCOA2 may be a cause of acute myeloid leukemias. Inversion inv(8)(p11;q13) generates the KAT6A-NCOA2 oncogene, which consists of the N-terminal part of KAT6A and the C-terminal part of NCOA2/TIF2. KAT6A-NCOA2 binds to CREBBP and disrupts its function in transcription activation. | ||
| + | == 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> [[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of the steroid binding domain (AF-2) but not of the modulating N-terminal domain (AF-1). Required with NCOA1 to control energy balance between white and brown adipose tissues.<ref>PMID:9430642</ref> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Boonmuen, N]] | ||
| + | [[Category: Bruno, N E]] | ||
| + | [[Category: Dharmarajan, V]] | ||
| + | [[Category: Frasor, J]] | ||
| + | [[Category: Goswami, D]] | ||
| + | [[Category: Griffin, P R]] | ||
[[Category: Kastrati, I]] | [[Category: Kastrati, I]] | ||
| - | [[Category: | + | [[Category: Katzenellenbogen, B S]] |
| + | [[Category: Katzenellenbogen, J A]] | ||
| + | [[Category: Min, J]] | ||
| + | [[Category: Nettles, K W]] | ||
[[Category: Novick, S]] | [[Category: Novick, S]] | ||
| - | [[Category: | + | [[Category: Nowak, J]] |
| - | [[Category: | + | [[Category: Nwachukwu, J C]] |
| - | + | ||
[[Category: Srinivasan, S]] | [[Category: Srinivasan, S]] | ||
| - | [[Category: Min, J]] | ||
| - | [[Category: Griffin, P.R]] | ||
| - | [[Category: Dharmarajan, V]] | ||
[[Category: Zhao, Y]] | [[Category: Zhao, Y]] | ||
| - | [[Category: | + | [[Category: Zhou, H B]] |
| - | [[Category: | + | [[Category: Ligand binding]] |
| - | [[Category: | + | [[Category: Nuclear receptor]] |
| - | [[Category: | + | [[Category: Protein-ligand complex]] |
| - | [[Category: | + | [[Category: Signaling protein]] |
| - | [[Category: | + | [[Category: Transcription]] |
| + | [[Category: Transcription factor]] | ||
Revision as of 19:25, 9 December 2016
Crystal Structure of the ER-alpha Ligand-binding Domain (Y537S) in Complex with an N-methyl, 2-chlorobenzyl OBHS-N derivative
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Categories: Boonmuen, N | Bruno, N E | Dharmarajan, V | Frasor, J | Goswami, D | Griffin, P R | Kastrati, I | Katzenellenbogen, B S | Katzenellenbogen, J A | Min, J | Nettles, K W | Novick, S | Nowak, J | Nwachukwu, J C | Srinivasan, S | Zhao, Y | Zhou, H B | Ligand binding | Nuclear receptor | Protein-ligand complex | Signaling protein | Transcription | Transcription factor
