4oq3
From Proteopedia
(Difference between revisions)
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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> | ||
- | </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>< | + | </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> |
- | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4dij|4dij]]</td></tr> | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4dij|4dij]]</td></tr> |
- | <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> | + | <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> |
- | <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> | + | <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> |
- | <table> | + | </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> | ||
- | From | + | From MEDLINE®/PubMed®, 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]] | ||
- | [[Category: Kallen, J | + | [[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
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