5acc: Difference between revisions

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'''Unreleased structure'''


The entry 5acc is ON HOLD
==A Novel Oral Selective Estrogen Receptor Down-regulator, AZD9496, drives Tumour Growth Inhibition in Estrogen Receptor positive and ESR1 Mutant Models==
<StructureSection load='5acc' size='340' side='right'caption='[[5acc]], [[Resolution|resolution]] 1.88&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5acc]] is a 1 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=5ACC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5ACC 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]] 1.88&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=KE9:(E)-3-(3,5-DIFLUORO-4-((1R,3R)-2-(2-FLUORO-2-+METHYLPROPYL)-3-METHYL-2,3,4,9-TETRAHYDRO-1H-PYRIDO(3,4-B)INDOL-1-YL)PHENYL)ACRYLIC+ACID'>KE9</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=5acc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5acc OCA], [https://pdbe.org/5acc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5acc RCSB], [https://www.ebi.ac.uk/pdbsum/5acc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5acc 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>


Authors: Norman, R.A., Weir, H.M., Bradbury, R.H., Lawson, M., Rabow, A.A., Buttar, D., Callis, R.J., Curwen, J.O., de Almeida, C., Ballard, P., Hulse, M., Donald, C.S., Feron, L.J.L., Gingell, H., Karoutchi, G., MacFaul, P., Moss, T., Pearson, S.E., Tonge, M., Davies, G., Walker, G.E., Wilson, Z., Rowlinson, R., Powell, S., Hemsley, P., Linney, E., Campbell, H., Ghazoui, Z., Sadler, C., Richmond, G., Pazolli, E., Mazzola, A.M., DCruz, C., De Savi, C.
==See Also==
 
*[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]]
Description: A Novel Oral Selective Estrogen Receptor Down-regulator, AZD9496, drives Tumour Growth Inhibition in Estrogen Receptor positive and ESR1 Mutant Models
== References ==
[[Category: Unreleased Structures]]
<references/>
[[Category: Campbell, H]]
__TOC__
[[Category: Powell, S]]
</StructureSection>
[[Category: Walker, G.E]]
[[Category: Homo sapiens]]
[[Category: Rabow, A.A]]
[[Category: Large Structures]]
[[Category: Hulse, M]]
[[Category: Ballard P]]
[[Category: Richmond, G]]
[[Category: Bradbury RH]]
[[Category: Wilson, Z]]
[[Category: Buttar D]]
[[Category: Curwen, J.O]]
[[Category: Callis RJ]]
[[Category: Moss, T]]
[[Category: Campbell H]]
[[Category: Karoutchi, G]]
[[Category: Curwen JO]]
[[Category: Lawson, M]]
[[Category: DCruz C]]
[[Category: Ballard, P]]
[[Category: Davies G]]
[[Category: De Almeida, C]]
[[Category: De Savi C]]
[[Category: Sadler, C]]
[[Category: Donald CS]]
[[Category: Davies, G]]
[[Category: Feron LJL]]
[[Category: Buttar, D]]
[[Category: Ghazoui Z]]
[[Category: Donald, C.S]]
[[Category: Gingell H]]
[[Category: Mazzola, A.M]]
[[Category: Hemsley P]]
[[Category: De Savi, C]]
[[Category: Hulse M]]
[[Category: Callis, R.J]]
[[Category: Karoutchi G]]
[[Category: Gingell, H]]
[[Category: Lawson M]]
[[Category: Rowlinson, R]]
[[Category: Linney E]]
[[Category: Macfaul, P]]
[[Category: MacFaul P]]
[[Category: Ghazoui, Z]]
[[Category: Mazzola AM]]
[[Category: Feron, L.J.L]]
[[Category: Moss T]]
[[Category: Norman, R.A]]
[[Category: Norman RA]]
[[Category: Weir, H.M]]
[[Category: Pazolli E]]
[[Category: Dcruz, C]]
[[Category: Pearson SE]]
[[Category: Linney, E]]
[[Category: Powell S]]
[[Category: Tonge, M]]
[[Category: Rabow AA]]
[[Category: Pazolli, E]]
[[Category: Richmond G]]
[[Category: Pearson, S.E]]
[[Category: Rowlinson R]]
[[Category: Bradbury, R.H]]
[[Category: Sadler C]]
[[Category: Hemsley, P]]
[[Category: Tonge M]]
[[Category: Walker GE]]
[[Category: Weir HM]]
[[Category: Wilson Z]]
[[Category: De Almeida C]]
Retrieved from "https://proteopedia.org/5acc"