4lwt: Difference between revisions
No edit summary |
No edit summary |
||
| Line 1: | Line 1: | ||
==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]] 1.60Å' scene=''> | <StructureSection load='4lwt' size='340' side='right' caption='[[4lwt]], [[Resolution|resolution]] 1.60Å' scene=''> | ||
| Line 5: | Line 6: | ||
</td></tr><tr id='ligand'><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></td></tr> | </td></tr><tr id='ligand'><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></td></tr> | ||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4lwu|4lwu]], [[4lwv|4lwv]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4lwu|4lwu]], [[4lwv|4lwv]]</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=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'>[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://pdbe.org/4lwt PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4lwt RCSB], [http://www.ebi.ac.uk/pdbsum/4lwt PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4lwt ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
| Line 17: | Line 18: | ||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 4lwt" style="background-color:#fffaf0;"></div> | |||
==See Also== | |||
*[[MDM2|MDM2]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 19:38, 5 August 2016
The 1.6A Crystal Structure of Humanized Xenopus MDM2 with RO5027344The 1.6A Crystal Structure of Humanized Xenopus MDM2 with RO5027344
Structural highlights
Function[MDM2_XENLA] E3 ubiquitin-protein ligase that mediates ubiquitination of p53/TP53, leading to its degration by the proteasome (By similarity). Publication Abstract from PubMedThe 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[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
|
| ||||||||||||||||||