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3omo
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==Fragment-Based Design of novel Estrogen Receptor Ligands== | ==Fragment-Based Design of novel Estrogen Receptor Ligands== | ||
| - | <StructureSection load='3omo' size='340' side='right' caption='[[3omo]], [[Resolution|resolution]] 2.21Å' scene=''> | + | <StructureSection load='3omo' size='340' side='right'caption='[[3omo]], [[Resolution|resolution]] 2.21Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[3omo]] is a 4 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[3omo]] 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=3OMO OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3OMO FirstGlance]. <br> |
| - | </td></tr><tr id=' | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.21Å</td></tr> |
| - | <tr id=' | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=WV7:2-(TRIFLUOROACETYL)-1,2,3,4-TETRAHYDROISOQUINOLIN-6-OL'>WV7</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=3omo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3omo OCA], [https://pdbe.org/3omo PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3omo RCSB], [https://www.ebi.ac.uk/pdbsum/3omo PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3omo ProSAT]</span></td></tr> | |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | |
</table> | </table> | ||
| - | == Disease == | ||
| - | [[http://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Note=A chromosomal aberration involving NCOA1 is a cause of rhabdomyosarcoma. Translocation t(2;2)(q35;p23) with PAX3 generates the NCOA1-PAX3 oncogene consisting of the N-terminus part of PAX3 and the C-terminus part of NCOA1. The fusion protein acts as a transcriptional activator. Rhabdomyosarcoma is the most common soft tissue carcinoma in childhood, representing 5-8% of all malignancies in children. | ||
== Function == | == Function == | ||
| - | [ | + | [https://www.uniprot.org/uniprot/ESR2_HUMAN ESR2_HUMAN] Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual. |
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==See Also== | ==See Also== | ||
| - | *[[Estrogen receptor|Estrogen receptor]] | + | *[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]] |
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: Brunsveld | + | [[Category: Large Structures]] |
| - | [[Category: | + | [[Category: Brunsveld L]] |
| - | [[Category: | + | [[Category: Dominguez Seoane M]] |
| - | [[Category: | + | [[Category: Fuchs S]] |
| - | [[Category: Ottmann | + | [[Category: Moecklinghoff S]] |
| - | [[Category: Rose | + | [[Category: Ottmann C]] |
| - | + | [[Category: Rose R]] | |
| - | [[Category: Waldmann | + | [[Category: Waldmann H]] |
| - | [[Category: | + | [[Category: Van Otterlo WA]] |
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Current revision
Fragment-Based Design of novel Estrogen Receptor Ligands
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