8c3n
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Stapled peptide SP30 in complex with humanised RadA mutant HumRadA22== | |
| + | <StructureSection load='8c3n' size='340' side='right'caption='[[8c3n]], [[Resolution|resolution]] 1.21Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[8c3n]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Pyrococcus_furiosus Pyrococcus furiosus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8C3N OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8C3N 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]] 1.21Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ADP:ADENOSINE-5-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=RF6:4,6-diethylpyrimidin-2-amine'>RF6</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=8c3n FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8c3n OCA], [https://pdbe.org/8c3n PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8c3n RCSB], [https://www.ebi.ac.uk/pdbsum/8c3n PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8c3n ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/RADA_PYRFU RADA_PYRFU] Involved in DNA repair and in homologous recombination. Binds and assemble on single-stranded DNA to form a nucleoprotein filament. Hydrolyzes ATP in a ssDNA-dependent manner and promotes DNA strand exchange between homologous DNA molecules. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Stapling is a macrocyclisation method that connects amino acid side chains of a peptide to improve its pharmacological properties. We describe an approach for stapled peptide preparation and biochemical evaluation that combines recombinant expression of fusion constructs of target peptides and cysteine-reactive divinyl-heteroaryl chemistry as an alternative to solid-phase synthesis. We then employ this workflow to prepare and evaluate BRC-repeat-derived inhibitors of the RAD51 recombinase, showing that a diverse range of secondary structure elements in the BRC repeat can be stapled without compromising binding and function. Using X-ray crystallography, we elucidate the atomic-level features of the staple moieties. We then demonstrate that BRC-repeat-derived stapled peptides can disrupt RAD51 function in cells following ionising radiation treatment. | ||
| - | + | A recombinant approach for stapled peptide discovery yields inhibitors of the RAD51 recombinase.,Pantelejevs T, Zuazua-Villar P, Koczy O, Counsell AJ, Walsh SJ, Robertson NS, Spring DR, Downs JA, Hyvonen M Chem Sci. 2023 Nov 21;14(47):13915-13923. doi: 10.1039/d3sc03331g. eCollection , 2023 Dec 6. PMID:38075664<ref>PMID:38075664</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: Hyvonen | + | <div class="pdbe-citations 8c3n" style="background-color:#fffaf0;"></div> |
| - | [[Category: Pantelejevs | + | == References == |
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Pyrococcus furiosus]] | ||
| + | [[Category: Hyvonen M]] | ||
| + | [[Category: Pantelejevs T]] | ||
Current revision
Stapled peptide SP30 in complex with humanised RadA mutant HumRadA22
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