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3w69

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<StructureSection load='3w69' size='340' side='right' caption='[[3w69]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
<StructureSection load='3w69' size='340' side='right' caption='[[3w69]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<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>
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<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>
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</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><br>
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</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>
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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>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glucokinase Glucokinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.2 2.7.1.2] </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=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>
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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=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>
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</table>
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<table>
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== 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>
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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>
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==See Also==
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*[[MDM2|MDM2]]
== References ==
== References ==
<references/>
<references/>
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</StructureSection>
</StructureSection>
[[Category: Human]]
[[Category: Human]]
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[[Category: Katakura, S.]]
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[[Category: Katakura, S]]
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[[Category: Kawato, H.]]
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[[Category: Kawato, H]]
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[[Category: Miyazaki, M.]]
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[[Category: Miyazaki, M]]
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[[Category: Naito, H.]]
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[[Category: Naito, H]]
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[[Category: Okayama, T.]]
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[[Category: Okayama, T]]
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[[Category: Shimizu, H.]]
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[[Category: Shimizu, H]]
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[[Category: Soga, T.]]
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[[Category: Soga, T]]
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[[Category: Sugimoto, Y.]]
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[[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]]

Revision as of 10:49, 4 January 2015

Crystal structure of human mdm2 with a dihydroimidazothiazole inhibitor

3w69, resolution 1.90Å

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