5c5a

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'''Unreleased structure'''
 
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The entry 5c5a is ON HOLD until Paper Publication
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==Crystal Structure of HDM2 in complex with Nutlin-3a==
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<StructureSection load='5c5a' size='340' side='right'caption='[[5c5a]], [[Resolution|resolution]] 1.15&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5c5a]] is a 2 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=5C5A OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5C5A FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.146&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene>, <scene name='pdbligand=NUT:4-({(4S,5R)-4,5-BIS(4-CHLOROPHENYL)-2-[4-METHOXY-2-(PROPAN-2-YLOXY)PHENYL]-4,5-DIHYDRO-1H-IMIDAZOL-1-YL}CARBONYL)PIPERAZIN-2-ONE'>NUT</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5c5a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5c5a OCA], [https://pdbe.org/5c5a PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5c5a RCSB], [https://www.ebi.ac.uk/pdbsum/5c5a PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5c5a ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/MDM2_HUMAN MDM2_HUMAN] Note=Seems to be amplified in certain tumors (including soft tissue sarcomas, osteosarcomas and gliomas). A higher frequency of splice variants lacking p53 binding domain sequences was found in late-stage and high-grade ovarian and bladder carcinomas. Four of the splice variants show loss of p53 binding.
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== Function ==
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[https://www.uniprot.org/uniprot/MDM2_HUMAN MDM2_HUMAN] E3 ubiquitin-protein ligase that mediates ubiquitination of p53/TP53, leading to its degradation by the proteasome. Inhibits p53/TP53- and p73/TP73-mediated cell cycle arrest and apoptosis by binding its transcriptional activation domain. Also acts as an ubiquitin ligase E3 toward itself and ARRB1. Permits the nuclear export of p53/TP53. Promotes proteasome-dependent ubiquitin-independent degradation of retinoblastoma RB1 protein. Inhibits DAXX-mediated apoptosis by inducing its ubiquitination and degradation. Component of the TRIM28/KAP1-MDM2-p53/TP53 complex involved in stabilizing p53/TP53. Also component of the TRIM28/KAP1-ERBB4-MDM2 complex which links growth factor and DNA damage response pathways. Mediates ubiquitination and subsequent proteasome degradation of DYRK2 in nucleus. Ubiquitinates IGF1R and promotes it to proteasomal degradation.<ref>PMID:12821780</ref> <ref>PMID:15053880</ref> <ref>PMID:15195100</ref> <ref>PMID:16337594</ref> <ref>PMID:15632057</ref> <ref>PMID:17290220</ref> <ref>PMID:19098711</ref> <ref>PMID:19219073</ref> <ref>PMID:19965871</ref> <ref>PMID:20858735</ref> <ref>PMID:20173098</ref>
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Authors: Orts, J., Waelti, M.A., Marsh, M., Vera, L., Gossert, A.D., Guentert, P., Riek, R.
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==See Also==
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*[[MDM2 3D structures|MDM2 3D structures]]
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Description: Crystal Structure of HDM2 in complex with Nutlin-3a
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== References ==
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[[Category: Unreleased Structures]]
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<references/>
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[[Category: Waelti, M.A]]
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__TOC__
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[[Category: Marsh, M]]
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</StructureSection>
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[[Category: Riek, R]]
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[[Category: Homo sapiens]]
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[[Category: Orts, J]]
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[[Category: Large Structures]]
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[[Category: Vera, L]]
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[[Category: Gossert AD]]
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[[Category: Guentert, P]]
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[[Category: Guentert P]]
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[[Category: Gossert, A.D]]
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[[Category: Marsh M]]
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[[Category: Orts J]]
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[[Category: Riek R]]
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[[Category: Vera L]]
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[[Category: Waelti MA]]

Current revision

Crystal Structure of HDM2 in complex with Nutlin-3a

PDB ID 5c5a

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