View source for 7elg


==LC3B modificated with a covalent probe==
<StructureSection load='7elg' size='340' side='right'caption='[[7elg]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7ELG OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7ELG 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]] 1.599&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=8Z6:2-methylidene-5-thiophen-2-yl-cyclohexane-1,3-dione'>8Z6</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'>[https://proteopedia.org/fgij/fg.htm?mol=7elg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7elg OCA], [https://pdbe.org/7elg PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7elg RCSB], [https://www.ebi.ac.uk/pdbsum/7elg PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7elg ProSAT]</span></td></tr>
</table>
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== Publication Abstract from PubMed ==
The autophagic ubiquitin-like protein LC3 functions through interactions with LC3-interaction regions (LIRs) of other autophagy proteins including autophagy receptors, which stands out as a promising protein-protein interaction (PPI) target for the intervention of autophagy. Post-translational modifications like acetylation of Lys49 on the LIR-interacting surface could disrupt the interaction, offering an opportunity to design covalent small molecules interfering the interface. Through screening covalent compounds, we discover a small molecule modulator of LC3A/B that covalently modifies LC3A/B protein at Lys49. Activity-based protein profiling (ABPP) based evaluations reveal that a derivative molecule DC-LC3in-D5 exhibits a potent covalent reactivity and selectivity to LC3A/B in HeLa cells. DC-LC3in-D5 compromises LC3B lipidation in vitro and in HeLa cells, leading to deficiency in the formation of autophagic structures and autophagic substrate degradation. DC-LC3in-D5 could serve as a powerful tool for autophagy research as well as for therapeutic interventions.

Inhibition of autophagy by a small molecule through covalent modification of LC3.,Luo C, Fan S, Yue L, Wan W, Zhang Y, Zhang B, Otomo C, Li Q, Lin T, Hu J, Xu P, Zhu M, Tao H, Chen Z, Li L, Ding H, Yao Z, Lu J, Wen Y, Zhang N, Tan M, Chen K, Xie Y, Otomo T, Zhou B, Jiang H, Dang Y Angew Chem Int Ed Engl. 2021 Sep 29. doi: 10.1002/anie.202109464. PMID:34590387<ref>PMID:34590387</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 7elg" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Large Structures]]
[[Category: Fan S]]
[[Category: Wan W]]