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==The 1.6A Crystal Structure of Humanized Xenopus MDM2 with RO5027344==
==The 1.6A Crystal Structure of Humanized Xenopus MDM2 with RO5027344==
<StructureSection load='4lwt' size='340' side='right' caption='[[4lwt]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
<StructureSection load='4lwt' size='340' side='right'caption='[[4lwt]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[4lwt]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LWT OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4LWT FirstGlance]. <br>
<table><tr><td colspan='2'>[[4lwt]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LWT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4LWT FirstGlance]. <br>
</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=20Q:(3S)-3-[(3R)-1-ACETYLPIPERIDIN-3-YL]-6-CHLORO-3-(3-CHLOROBENZYL)-1,3-DIHYDRO-2H-INDOL-2-ONE'>20Q</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene><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]] 1.6&#8491;</td></tr>
<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4lwu|4lwu]], [[4lwv|4lwv]]</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=20Q:(3S)-3-[(3R)-1-ACETYLPIPERIDIN-3-YL]-6-CHLORO-3-(3-CHLOROBENZYL)-1,3-DIHYDRO-2H-INDOL-2-ONE'>20Q</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4lwt FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lwt OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4lwt RCSB], [http://www.ebi.ac.uk/pdbsum/4lwt PDBsum]</span></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=4lwt FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lwt OCA], [https://pdbe.org/4lwt PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4lwt RCSB], [https://www.ebi.ac.uk/pdbsum/4lwt PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4lwt ProSAT]</span></td></tr>
<table>
</table>
<div style="background-color:#fffaf0;">
== Function ==
== Publication Abstract from PubMed ==
[https://www.uniprot.org/uniprot/MDM2_XENLA MDM2_XENLA] E3 ubiquitin-protein ligase that mediates ubiquitination of p53/TP53, leading to its degration by the proteasome (By similarity).
The field of small-molecule inhibitors of protein-protein interactions is rapidly advancing and the specific area of inhibitors of the p53/MDM2 interaction is a prime example. Several groups have published on this topic and multiple compounds are in various stages of clinical development. Building on the strength of the discovery of RG7112, a Nutlin imidazoline-based compound, and RG7388, a pyrrolidine-based compound, we have developed additional scaffolds that provide opportunities for future development. Here, we report the discovery and optimization of a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitors, culminating in RO8994.
 
Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.,Zhang Z, Ding Q, Liu JJ, Zhang J, Jiang N, Chu XJ, Bartkovitz D, Luk KC, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B Bioorg Med Chem. 2014 Jun 11. pii: S0968-0896(14)00431-3. doi:, 10.1016/j.bmc.2014.05.072. PMID:24997575<ref>PMID:24997575</ref>


From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
==See Also==
</div>
*[[MDM2 3D structures|MDM2 3D structures]]
== References ==
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Graves, B J.]]
[[Category: Large Structures]]
[[Category: Kammlott, U.]]
[[Category: Xenopus laevis]]
[[Category: Lukacs, C.]]
[[Category: Graves BJ]]
[[Category: E3 ubiquitin ligase]]
[[Category: Kammlott U]]
[[Category: Indolinone]]
[[Category: Lukacs C]]
[[Category: Ligase-ligase inhibitor complex]]
[[Category: Mdm2]]
[[Category: Nucleus]]
[[Category: P53]]

Latest revision as of 15:22, 1 March 2024

The 1.6A Crystal Structure of Humanized Xenopus MDM2 with RO5027344The 1.6A Crystal Structure of Humanized Xenopus MDM2 with RO5027344

Structural highlights

4lwt is a 1 chain structure with sequence from Xenopus laevis. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.6Å
Ligands:,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

MDM2_XENLA E3 ubiquitin-protein ligase that mediates ubiquitination of p53/TP53, leading to its degration by the proteasome (By similarity).

See Also

4lwt, resolution 1.60Å

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