5ngz
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Ube2T in complex with fragment EM04== | |
| + | <StructureSection load='5ngz' size='340' side='right' caption='[[5ngz]], [[Resolution|resolution]] 2.40Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5ngz]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5NGZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5NGZ FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2BG:1-(1,3-BENZOTHIAZOL-2-YL)METHANAMINE'>2BG</scene></td></tr> | ||
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/E2_ubiquitin-conjugating_enzyme E2 ubiquitin-conjugating enzyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.2.23 2.3.2.23] </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=5ngz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ngz OCA], [http://pdbe.org/5ngz PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5ngz RCSB], [http://www.ebi.ac.uk/pdbsum/5ngz PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5ngz ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/UBE2T_HUMAN UBE2T_HUMAN]] Accepts ubiquitin from the E1 complex and catalyzes its covalent attachment to other proteins. Catalyzes monoubiquitination. Involved in mitomycin-C (MMC)-induced DNA repair: acts as a specific E2 ubiquitin-conjugating enzyme for the Fanconi anemia complex by associating with E3 ubiquitin-protein ligase FANCL and catalyzing monoubiquitination of FANCD2, a key step in the DNA damage pathway. Also mediates monoubiquitination of FANCL and FANCI. May contribute to ubiquitination and degradation of BRCA1. In vitro able to promote polyubiquitination using all 7 ubiquitin Lys residues, but may prefer 'Lys-11'-, 'Lys-27'-, 'Lys-48'- and 'Lys-63'-linked polyubiquitination.<ref>PMID:16916645</ref> <ref>PMID:17938197</ref> <ref>PMID:19111657</ref> <ref>PMID:19887602</ref> <ref>PMID:19589784</ref> <ref>PMID:20061386</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Ube2T is the E2 ubiquitin-conjugating enzyme of the Fanconi anemia DNA repair pathway and it is overexpressed in several cancers, representing an attractive target for the development of inhibitors. Despite the extensive efforts in targeting the ubiquitin system, very few E2 binders have currently been discovered. Herein we report the identification of a new allosteric pocket on Ube2T through a fragment screening using biophysical methods. Several fragments binding to this site inhibit ubiquitin conjugation in vitro. | ||
| - | + | Allosteric Targeting of the Fanconi Anemia Ubiquitin-Conjugating Enzyme Ube2T by Fragment Screening.,Morreale FE, Bortoluzzi A, Chaugule VK, Arkinson C, Walden H, Ciulli A J Med Chem. 2017 May 2. doi: 10.1021/acs.jmedchem.7b00147. PMID:28437106<ref>PMID:28437106</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| + | <div class="pdbe-citations 5ngz" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: E2 ubiquitin-conjugating enzyme]] | ||
| + | [[Category: Arkinson, C]] | ||
| + | [[Category: Bortoluzzi, A]] | ||
| + | [[Category: Chaugule, V K]] | ||
| + | [[Category: Ciulli, A]] | ||
| + | [[Category: Morreale, F E]] | ||
| + | [[Category: Walden, H]] | ||
| + | [[Category: Dna repair]] | ||
| + | [[Category: Fanconi anemia pathway]] | ||
| + | [[Category: Fragment screening]] | ||
| + | [[Category: Ligase]] | ||
| + | [[Category: Ubiquitin-conjugating enzyme ube2t]] | ||
Revision as of 13:02, 4 May 2017
Ube2T in complex with fragment EM04
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