This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.


4lwv

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Current revision (12:22, 1 March 2024) (edit) (undo)
 
(3 intermediate revisions not shown.)
Line 1: Line 1:
 +
==The 2.3A Crystal Structure of Humanized Xenopus MDM2 with RO5545353==
==The 2.3A Crystal Structure of Humanized Xenopus MDM2 with RO5545353==
-
<StructureSection load='4lwv' size='340' side='right' caption='[[4lwv]], [[Resolution|resolution]] 2.32&Aring;' scene=''>
+
<StructureSection load='4lwv' size='340' side='right'caption='[[4lwv]], [[Resolution|resolution]] 2.32&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
-
<table><tr><td colspan='2'>[[4lwv]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LWV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4LWV FirstGlance]. <br>
+
<table><tr><td colspan='2'>[[4lwv]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LWV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4LWV FirstGlance]. <br>
-
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=20W:(2S,3R,4R,5R)-N-(4-CARBAMOYL-2-METHOXYPHENYL)-2-CHLORO-4-(3-CHLORO-2-FLUOROPHENYL)-2-(2,2-DIMETHYLPROPYL)-5-OXO-4,5-DIHYDROSPIRO[PYRROLIDINE-3,6-THIENO[3,2-B]PYRROLE]-5-CARBOXAMIDE'>20W</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
+
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.32&#8491;</td></tr>
-
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4lwt|4lwt]], [[4lwu|4lwu]]</td></tr>
+
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=20W:(2S,3R,4R,5R)-N-(4-CARBAMOYL-2-METHOXYPHENYL)-2-CHLORO-4-(3-CHLORO-2-FLUOROPHENYL)-2-(2,2-DIMETHYLPROPYL)-5-OXO-4,5-DIHYDROSPIRO[PYRROLIDINE-3,6-THIENO[3,2-B]PYRROLE]-5-CARBOXAMIDE'>20W</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></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=4lwv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lwv OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4lwv RCSB], [http://www.ebi.ac.uk/pdbsum/4lwv PDBsum]</span></td></tr>
+
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4lwv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lwv OCA], [https://pdbe.org/4lwv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4lwv RCSB], [https://www.ebi.ac.uk/pdbsum/4lwv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4lwv ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== 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).
+
[https://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;">
+
-
== Publication Abstract from PubMed ==
+
-
The development of small-molecule MDM2 inhibitors to restore dysfunctional p53 activities represents a novel approach for cancer treatment. In a previous communication, the efforts leading to the identification of a non-imidazoline MDM2 inhibitor, RG7388, was disclosed and revealed the desirable in vitro and in vivo pharmacological properties that this class of pyrrolidine-based inhibitors possesses. Given this richness and the critical need for a wide variety of chemical structures to ensure success in the clinic, research was expanded to evaluate additional derivatives. Here we report two new potent, selective, and orally active p53-MDM2 antagonists, RO5353 and RO2468, as follow-ups with promising potential for clinical development.
+
-
 
+
-
Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.,Zhang Z, Chu XJ, Liu JJ, Ding Q, Zhang J, Bartkovitz D, Jiang N, Karnachi P, So SS, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev L, Graves B ACS Med Chem Lett. 2013 Dec 29;5(2):124-7. doi: 10.1021/ml400359z. eCollection, 2014 Feb 13. PMID:24900784<ref>PMID:24900784</ref>
+
-
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+
==See Also==
-
</div>
+
*[[MDM2 3D structures|MDM2 3D structures]]
-
== References ==
+
-
<references/>
+
__TOC__
__TOC__
</StructureSection>
</StructureSection>
-
[[Category: Graves, B J]]
+
[[Category: Large Structures]]
-
[[Category: Janson, C A]]
+
[[Category: Xenopus laevis]]
-
[[Category: Lukacs, C]]
+
[[Category: Graves BJ]]
-
[[Category: E3 ubiquitin ligase]]
+
[[Category: Janson CA]]
-
[[Category: Ligase-ligase inhibitor complex]]
+
[[Category: Lukacs C]]
-
[[Category: Mdm2]]
+
-
[[Category: Nucleus]]
+
-
[[Category: P53]]
+

Current revision

The 2.3A Crystal Structure of Humanized Xenopus MDM2 with RO5545353

PDB ID 4lwv

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4lwv"
Personal tools