4oq3

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== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[4oq3]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4OQ3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4OQ3 FirstGlance]. <br>
<table><tr><td colspan='2'>[[4oq3]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4OQ3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4OQ3 FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2V8:1-(5-CHLORO-2-METHYLPHENYL)-5-(3-CHLOROPHENYL)-2-(3-METHYLPHENYL)-1H-IMIDAZOLE-4-CARBOXYLIC+ACID'>2V8</scene><br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2V8:1-(5-CHLORO-2-METHYLPHENYL)-5-(3-CHLOROPHENYL)-2-(3-METHYLPHENYL)-1H-IMIDAZOLE-4-CARBOXYLIC+ACID'>2V8</scene></td></tr>
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<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4dij|4dij]]</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4dij|4dij]]</td></tr>
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<tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">MDM2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">MDM2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
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<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=4oq3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oq3 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4oq3 RCSB], [http://www.ebi.ac.uk/pdbsum/4oq3 PDBsum]</span></td></tr>
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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=4oq3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oq3 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4oq3 RCSB], [http://www.ebi.ac.uk/pdbsum/4oq3 PDBsum]</span></td></tr>
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<table>
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</table>
== Disease ==
== Disease ==
[[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.
[[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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Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction.,Vaupel A, Bold G, De Pover A, Stachyra-Valat T, Hergovich-Lisztwan J, Kallen J, Masuya K, Furet P Bioorg Med Chem Lett. 2014 May 1;24(9):2110-4. doi: 10.1016/j.bmcl.2014.03.039., Epub 2014 Mar 22. PMID:24704029<ref>PMID:24704029</ref>
Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction.,Vaupel A, Bold G, De Pover A, Stachyra-Valat T, Hergovich-Lisztwan J, Kallen J, Masuya K, Furet P Bioorg Med Chem Lett. 2014 May 1;24(9):2110-4. doi: 10.1016/j.bmcl.2014.03.039., Epub 2014 Mar 22. PMID:24704029<ref>PMID:24704029</ref>
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
</div>
== References ==
== References ==
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</StructureSection>
</StructureSection>
[[Category: Human]]
[[Category: Human]]
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[[Category: Kallen, J.]]
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[[Category: Kallen, J]]
[[Category: Inhibitor complex]]
[[Category: Inhibitor complex]]
[[Category: Ligase-ligase inhibitor complex]]
[[Category: Ligase-ligase inhibitor complex]]
[[Category: Ppi with p53]]
[[Category: Ppi with p53]]

Revision as of 09:44, 5 January 2015

Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction

4oq3, resolution 2.30Å

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