3w69: Difference between revisions
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<StructureSection load='3w69' size='340' side='right' caption='[[3w69]], [[Resolution|resolution]] 1.90Å' scene=''> | <StructureSection load='3w69' size='340' side='right' caption='[[3w69]], [[Resolution|resolution]] 1.90Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[3w69]] is a 2 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=3W69 OCA]. <br> | <table><tr><td colspan='2'>[[3w69]] is a 2 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=3W69 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3W69 FirstGlance]. <br> | ||
</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LTZ:(5R,6S)-2-[((2S,5R)-2-{[(3R)-4-ACETYL-3-METHYLPIPERAZIN-1-YL]CARBONYL}-5-ETHYLPYRROLIDIN-1-YL)CARBONYL]-5,6-BIS(4-CHLOROPHENYL)-3-ISOPROPYL-6-METHYL-5,6-DIHYDROIMIDAZO[2,1-B][1,3]THIAZOLE'>LTZ</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>< | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LTZ:(5R,6S)-2-[((2S,5R)-2-{[(3R)-4-ACETYL-3-METHYLPIPERAZIN-1-YL]CARBONYL}-5-ETHYLPYRROLIDIN-1-YL)CARBONYL]-5,6-BIS(4-CHLOROPHENYL)-3-ISOPROPYL-6-METHYL-5,6-DIHYDROIMIDAZO[2,1-B][1,3]THIAZOLE'>LTZ</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></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 | <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=3w69 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3w69 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3w69 RCSB], [http://www.ebi.ac.uk/pdbsum/3w69 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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Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors.,Miyazaki M, Naito H, Sugimoto Y, Yoshida K, Kawato H, Okayama T, Shimizu H, Miyazaki M, Kitagawa M, Seki T, Fukutake S, Shiose Y, Aonuma M, Soga T Bioorg Med Chem. 2013 Jul 15;21(14):4319-31. doi: 10.1016/j.bmc.2013.04.056. Epub, 2013 Apr 30. PMID:23685175<ref>PMID:23685175</ref> | Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors.,Miyazaki M, Naito H, Sugimoto Y, Yoshida K, Kawato H, Okayama T, Shimizu H, Miyazaki M, Kitagawa M, Seki T, Fukutake S, Shiose Y, Aonuma M, Soga T Bioorg Med Chem. 2013 Jul 15;21(14):4319-31. doi: 10.1016/j.bmc.2013.04.056. Epub, 2013 Apr 30. PMID:23685175<ref>PMID:23685175</ref> | ||
From | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
==See Also== | |||
*[[MDM2|MDM2]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
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</StructureSection> | </StructureSection> | ||
[[Category: Human]] | [[Category: Human]] | ||
[[Category: Katakura, S | [[Category: Katakura, S]] | ||
[[Category: Kawato, H | [[Category: Kawato, H]] | ||
[[Category: Miyazaki, M | [[Category: Miyazaki, M]] | ||
[[Category: Naito, H | [[Category: Naito, H]] | ||
[[Category: Okayama, T | [[Category: Okayama, T]] | ||
[[Category: Shimizu, H | [[Category: Shimizu, H]] | ||
[[Category: Soga, T | [[Category: Soga, T]] | ||
[[Category: Sugimoto, Y | [[Category: Sugimoto, Y]] | ||
[[Category: Ligase-ligase inhibitor complex]] | [[Category: Ligase-ligase inhibitor complex]] | ||
[[Category: P53]] | [[Category: P53]] | ||
[[Category: Ubiquitin-protein ligase e3 mdm2]] | [[Category: Ubiquitin-protein ligase e3 mdm2]] | ||
