5zxf

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'''Unreleased structure'''
 
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The entry 5zxf is ON HOLD
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==The 1.25A Crystal structure of His6-tagged Mdm2 in complex with nutlin-3a==
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<StructureSection load='5zxf' size='340' side='right' caption='[[5zxf]], [[Resolution|resolution]] 1.25&Aring;' scene=''>
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Authors: Cheng, X.Y., Su, Z.D., Pi, N., Cao, C.Z., Zhao, Z.T., Zhou, J.J., Chen, R., Kuang, Z.K., Huang, Y.Q.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5zxf]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5ZXF OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5ZXF FirstGlance]. <br>
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Description: The 1.25A Crystal structure of His6-tagged Mdm2 in complex with nutlin-3a
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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></td></tr>
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[[Category: Unreleased Structures]]
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/RING-type_E3_ubiquitin_transferase RING-type E3 ubiquitin transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.2.27 2.3.2.27] </span></td></tr>
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[[Category: Huang, Y.Q]]
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5zxf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5zxf OCA], [http://pdbe.org/5zxf PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5zxf RCSB], [http://www.ebi.ac.uk/pdbsum/5zxf PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5zxf ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[[http://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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[[http://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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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: RING-type E3 ubiquitin transferase]]
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[[Category: Cao, C Z]]
[[Category: Chen, R]]
[[Category: Chen, R]]
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[[Category: Cao, C.Z]]
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[[Category: Cheng, X Y]]
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[[Category: Huang, Y Q]]
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[[Category: Kuang, Z K]]
[[Category: Pi, N]]
[[Category: Pi, N]]
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[[Category: Zhao, Z.T]]
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[[Category: Su, Z D]]
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[[Category: Kuang, Z.K]]
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[[Category: Zhao, Z T]]
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[[Category: Cheng, X.Y]]
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[[Category: Zhou, J J]]
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[[Category: Zhou, J.J]]
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[[Category: Cell cycle]]
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[[Category: Su, Z.D]]
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[[Category: P53]]

Revision as of 06:02, 22 August 2018

The 1.25A Crystal structure of His6-tagged Mdm2 in complex with nutlin-3a

5zxf, resolution 1.25Å

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