3tpx

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[[Image:3tpx.png|left|200px]]
 
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{{STRUCTURE_3tpx| PDB=3tpx | SCENE= }}
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==Crystal structure of human MDM2 in complex with a trifluoromethylated D-peptide inhibitor==
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<StructureSection load='3tpx' size='340' side='right'caption='[[3tpx]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3tpx]] is a 6 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=3TPX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3TPX 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]] 1.8&#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=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=DAL:D-ALANINE'>DAL</scene>, <scene name='pdbligand=DAR:D-ARGININE'>DAR</scene>, <scene name='pdbligand=DGL:D-GLUTAMIC+ACID'>DGL</scene>, <scene name='pdbligand=DLE:D-LEUCINE'>DLE</scene>, <scene name='pdbligand=DLY:D-LYSINE'>DLY</scene>, <scene name='pdbligand=DSG:D-ASPARAGINE'>DSG</scene>, <scene name='pdbligand=DTH:D-THREONINE'>DTH</scene>, <scene name='pdbligand=DTR:D-TRYPTOPHAN'>DTR</scene>, <scene name='pdbligand=DTY:D-TYROSINE'>DTY</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=TDF:4-(TRIFLUOROMETHYL)-D-PHENYLALANINE'>TDF</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=3tpx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3tpx OCA], [https://pdbe.org/3tpx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3tpx RCSB], [https://www.ebi.ac.uk/pdbsum/3tpx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3tpx 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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===Crystal structure of human MDM2 in complex with a trifluoromethylated D-peptide inhibitor===
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==See Also==
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*[[MDM2 3D structures|MDM2 3D structures]]
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{{ABSTRACT_PUBMED_22694121}}
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== References ==
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<references/>
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==About this Structure==
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__TOC__
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[[3tpx]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3TPX OCA].
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</StructureSection>
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[[Category: Homo sapiens]]
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==Reference==
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[[Category: Large Structures]]
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<ref group="xtra">PMID:022694121</ref><references group="xtra"/>
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[[Category: Pazgier M]]
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[[Category: Pazgier, M.]]
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[[Category: Wu X]]
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[[Category: Wu, X.]]
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[[Category: Ligase-ligase inhibitor complex]]
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[[Category: Mdm2-d-peptide inhibitor complex]]
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[[Category: P53-binding domain of mdm2-d-peptide inhibitor complex]]
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Current revision

Crystal structure of human MDM2 in complex with a trifluoromethylated D-peptide inhibitor

PDB ID 3tpx

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