5o6s
From Proteopedia
(Difference between revisions)
(New page: '''Unreleased structure''' The entry 5o6s is ON HOLD until Paper Publication Authors: Gabrielsen, M., Buetow, L., Huang, D.T. Description: UbV.B4R, a dimeric ubiquitin variant binding ...) |
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| - | '''Unreleased structure''' | ||
| - | + | ==UbV.B4R, a dimeric ubiquitin variant binding to BIRC4 RING== | |
| + | <StructureSection load='5o6s' size='340' side='right'caption='[[5o6s]], [[Resolution|resolution]] 2.90Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5o6s]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5O6S OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5O6S FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.9Å</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=5o6s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5o6s OCA], [https://pdbe.org/5o6s PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5o6s RCSB], [https://www.ebi.ac.uk/pdbsum/5o6s PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5o6s ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | RING and U-box E3 ubiquitin ligases regulate diverse eukaryotic processes and have been implicated in numerous diseases, but targeting these enzymes remains a major challenge. We report the development of three ubiquitin variants (UbVs), each binding selectively to the RING or U-box domain of a distinct E3 ligase: monomeric UBE4B, phosphorylated active CBL, or dimeric XIAP. Structural and biochemical analyses revealed that UbVs specifically inhibited the activity of UBE4B or phosphorylated CBL by blocking the E2 approximately Ub binding site. Surprisingly, the UbV selective for dimeric XIAP formed a dimer to stimulate E3 activity by stabilizing the closed E2 approximately Ub conformation. We further verified the inhibitory and stimulatory functions of UbVs in cells. Our work provides a general strategy to inhibit or activate RING/U-box E3 ligases and provides a resource for the research community to modulate these enzymes. | ||
| - | + | A General Strategy for Discovery of Inhibitors and Activators of RING and U-box E3 Ligases with Ubiquitin Variants.,Gabrielsen M, Buetow L, Nakasone MA, Ahmed SF, Sibbet GJ, Smith BO, Zhang W, Sidhu SS, Huang DT Mol Cell. 2017 Oct 19;68(2):456-470.e10. doi: 10.1016/j.molcel.2017.09.027. PMID:29053960<ref>PMID:29053960</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: | + | <div class="pdbe-citations 5o6s" style="background-color:#fffaf0;"></div> |
| - | [[Category: Gabrielsen | + | == References == |
| - | [[Category: | + | <references/> |
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Buetow L]] | ||
| + | [[Category: Gabrielsen M]] | ||
| + | [[Category: Huang DT]] | ||
Current revision
UbV.B4R, a dimeric ubiquitin variant binding to BIRC4 RING
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