6iq4

Nucleosome core particle cross-linked with a hetero-binuclear molecule possessing RAPTA and gold(I) 4-(diphenylphosphino)benzoic acid groups.

spinqualitylabelsall models 6iq4, resolution 2.25Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 6iq4 is a 10 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.25Å Ligands: AU, MG, XIS Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function H31_HUMAN Publication Abstract from PubMed Targeting defined histone protein sites in chromatin is an emerging therapeutic approach that can potentially be enhanced by allosteric effects within the nucleosome. Here we characterized a novel hetero-bimetallic compound with a design based on a nucleosomal allostery effect observed earlier for two unrelated drugs-the Ru(II) antimetastasis/antitumor RAPTA-T and the Au(I) anti-arthritic auranofin. The Ru(II) moiety binds specifically to two H2A glutamate residues on the nucleosome acidic patch, allosterically triggering a cascade of structural changes that promote binding of the Au(I) moiety to selective histidine residues on H3, resulting in cross-linking sites that are over 35 A distant. By tethering the H2A-H2B dimers to the H3-H4 tetramer, the hetero-bimetallic compound significantly increases stability of the nucleosome, illustrating its utility as a site-selective cross-linking agent. Crosslinking Allosteric Sites on the Nucleosome.,Batchelor LK, De Falco L, von Erlach T, Sharma D, Adhireksan Z, Roethlisberger U, Davey CA, Dyson PJ Angew Chem Int Ed Engl. 2019 Oct 28;58(44):15660-15664. doi:, 10.1002/anie.201906423. Epub 2019 Sep 18. PMID:31478581 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Histone 3D structures

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