8c3n | pdb_00008c3n

Stapled peptide SP30 in complex with humanised RadA mutant HumRadA22

spinqualitylabelsall models 8c3n, resolution 1.21Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 8c3n is a 2 chain structure with sequence from Homo sapiens and Pyrococcus furiosus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 1.21Å Ligands: ADP, MG, RF6 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function 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. 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 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

Proteopedia Page Contributors and Editors (what is this?)

OCA