4j3e: Difference between revisions
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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=4j3e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4j3e OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4j3e RCSB], [http://www.ebi.ac.uk/pdbsum/4j3e 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=4j3e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4j3e OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4j3e RCSB], [http://www.ebi.ac.uk/pdbsum/4j3e PDBsum]</span></td></tr> | ||
</table> | </table> | ||
== Function == | |||
[[http://www.uniprot.org/uniprot/MDM2_XENLA MDM2_XENLA]] E3 ubiquitin-protein ligase that mediates ubiquitination of p53/TP53, leading to its degration by the proteasome (By similarity). | |||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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</StructureSection> | </StructureSection> | ||
[[Category: African clawed frog]] | [[Category: African clawed frog]] | ||
[[Category: Crowther, R | [[Category: Crowther, R]] | ||
[[Category: Graves, B J | [[Category: Graves, B J]] | ||
[[Category: Kammlott, R U | [[Category: Kammlott, R U]] | ||
[[Category: Lukacs, C M | [[Category: Lukacs, C M]] | ||
[[Category: E3 ubiquitin ligase]] | [[Category: E3 ubiquitin ligase]] | ||
[[Category: Imidazoline]] | [[Category: Imidazoline]] | ||
Revision as of 04:15, 25 December 2014
The 1.9A crystal structure of humanized Xenopus Mdm2 with nutlin-3aThe 1.9A crystal structure of humanized Xenopus Mdm2 with nutlin-3a
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 p53 tumor suppressor is a potent transcription factor that plays a key role in the regulation of cellular responses to stress. It is controlled by its negative regulator MDM2, which binds directly to p53 and inhibits its transcriptional activity. MDM2 also targets p53 for degradation by the proteasome. Many tumors produce high levels of MDM2, thereby impairing p53 function. Restoration of p53 activity by inhibiting the p53-MDM2 interaction may represent a novel approach to cancer treatment. RG7112 (2g) is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. In cancer cells expressing wild-type p53, RG7112 stabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.,Vu B, Wovkulich P, Pizzolato G, Lovey A, Ding Q, Jiang N, Liu JJ, Zhao C, Glenn K, Wen Y, Tovar C, Packman K, Vassilev L, Graves B ACS Med Chem Lett. 2013 Apr 2;4(5):466-9. doi: 10.1021/ml4000657. eCollection, 2013 May 9. PMID:24900694[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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