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| - | | + | #REDIRECT [[5kcc]] This PDB entry is obsolete and replaced by 5kcc |
| - | ==Crystal Structure of the ER-alpha Ligand-binding Domain (Y537S) in Complex with Oxabicyclic Heptene Sulfonamide (OBHS-N)==
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| - | <StructureSection load='4zub' size='340' side='right' caption='[[4zub]], [[Resolution|resolution]] 2.39Å' scene=''>
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| - | == Structural highlights ==
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| - | <table><tr><td colspan='2'>[[4zub]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ZUB OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ZUB FirstGlance]. <br>
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| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=OB1:(1S,2R,4S)-5,6-BIS(4-HYDROXYPHENYL)-N-PHENYL-7-OXABICYCLO[2.2.1]HEPT-5-ENE-2-SULFONAMIDE'>OB1</scene></td></tr>
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| - | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4pp6|4pp6]], [[4zn7|4zn7]], [[4zn9|4zn9]], [[4znh|4znh]], [[4zns|4zns]], [[4znt|4znt]], [[4znu|4znu]], [[4znv|4znv]], [[4znw|4znw]], [[4zuc|4zuc]], [[4zwh|4zwh]], [[4zwk|4zwk]], [[5bnu|5bnu]], [[5bp6|5bp6]], [[5bpr|5bpr]], [[5bq4|5bq4]]</td></tr>
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| - | <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=4zub FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zub OCA], [http://pdbe.org/4zub PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4zub RCSB], [http://www.ebi.ac.uk/pdbsum/4zub PDBsum]</span></td></tr>
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| - | </table>
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| - | == Disease ==
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| - | [[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.
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| - | == Function ==
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| - | [[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>
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| - | == References ==
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| - | <references/>
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| - | __TOC__
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| - | </StructureSection>
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| - | [[Category: Carlson, K E]]
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| - | [[Category: Cavett, V]]
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| - | [[Category: Dong, C]]
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| - | [[Category: Elemento, O]]
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| - | [[Category: Houtman, R]]
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| - | [[Category: Josan, J S]]
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| - | [[Category: Katzenellenbogen, J A]]
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| - | [[Category: Liao, Z]]
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| - | [[Category: Min, J]]
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| - | [[Category: Nettles, K W]]
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| - | [[Category: Nowak, J]]
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| - | [[Category: Nwachukwu, J C]]
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| - | [[Category: Srinivasan, S]]
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| - | [[Category: Wang, S]]
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| - | [[Category: Zheng, Y]]
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| - | [[Category: Zhou, H B]]
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| - | [[Category: Ligand binding]]
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| - | [[Category: Nuclear receptor]]
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| - | [[Category: Protein-ligand complex]]
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| - | [[Category: Transcription]]
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| - | [[Category: Transcription factor]]
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