4pps

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m (Protected "4pps" [edit=sysop:move=sysop])
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'''Unreleased structure'''
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==Crystal Structure of the Estrogen Receptor alpha Ligand-binding Domain in Complex with an A-CD ring estrogen derivative==
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<StructureSection load='4pps' size='340' side='right' caption='[[4pps]], [[Resolution|resolution]] 1.93&Aring;' scene=''>
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The entry 4pps is ON HOLD until Paper Publication
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4pps]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4PPS OCA]. <br>
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Authors: Nwachukwu, J.C., Srinivasan, S., Bruno, N.E., Parent, A.A., Hughes, T.S., Pollock, J.A., Gjyshi, O., Cavett, V., Nowak, J., Garcia-Ordonez, R.D., Houtman, R., Griffin, P.R., Kojetin, D.J., Katzenellenbogen, J.A., Conkright, M.D., Nettles, K.W.
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ESE:(1S,3AR,5R,7AS)-5-(4-HYDROXYPHENYL)-7A-METHYLOCTAHYDRO-1H-INDEN-1-OL'>ESE</scene><br>
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<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4pp6|4pp6]], [[4ppp|4ppp]]</td></tr>
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Description: Crystal Structure of the Estrogen Receptor alpha Ligand-binding Domain in Complex with an A-CD ring estrogen derivative
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<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glucokinase Glucokinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.2 2.7.1.2] </span></td></tr>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4pps FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4pps OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4pps RCSB], [http://www.ebi.ac.uk/pdbsum/4pps 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: Bruno, N E.]]
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[[Category: Cavett, V.]]
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[[Category: Conkright, M D.]]
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[[Category: Garcia-Ordonez, R D.]]
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[[Category: Gjyshi, O.]]
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[[Category: Griffin, P R.]]
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[[Category: Houtman, R.]]
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[[Category: Hughes, T S.]]
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[[Category: Katzenellenbogen, J A.]]
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[[Category: Kojetin, D 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: Parent, A A.]]
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[[Category: Pollock, J A.]]
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[[Category: Srinivasan, S.]]
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[[Category: Ligand-binding]]
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[[Category: Nuclear hormone receptor]]
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[[Category: Nucleus]]
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[[Category: Protein binding]]
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[[Category: Transcription factor]]

Revision as of 08:24, 7 May 2014

Crystal Structure of the Estrogen Receptor alpha Ligand-binding Domain in Complex with an A-CD ring estrogen derivative

4pps, resolution 1.93Å

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