6dzr | pdb_00006dzr

Crystal structure of h38C2 K99R mutation

spinqualitylabelsall models 6dzr, resolution 2.40Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 6dzr is a 2 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: FLC, SO4 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Publication Abstract from PubMed Homogeneous antibody-drug conjugates (ADCs) that use a highly reactive buried lysine (Lys) residue embedded in a dual variable domain (DVD)-IgG1 format can be assembled with high precision and efficiency under mild conditions. Here we show that replacing the Lys with an arginine (Arg) residue affords an orthogonal ADC assembly that is site-selective and stable. X-ray crystallography confirmed the location of the reactive Arg residue at the bottom of a deep pocket. As the Lys-to-Arg mutation is confined to a single residue in the heavy chain of the DVD-IgG1, heterodimeric assemblies that combine a buried Lys in one arm, a buried Arg in the other arm, and identical light chains, are readily assembled. Furthermore, the orthogonal conjugation chemistry enables the loading of heterodimeric DVD-IgG1s with two different cargos in a one-pot reaction and thus affords a convenient platform for dual-warhead ADCs and other multifaceted antibody conjugates. Site-Selective Antibody Functionalization via Orthogonally Reactive Arginine and Lysine Residues.,Hwang D, Nilchan N, Nanna AR, Li X, Cameron MD, Roush WR, Park H, Rader C Cell Chem Biol. 2019 Jun 11. pii: S2451-9456(19)30179-5. doi:, 10.1016/j.chembiol.2019.05.010. PMID:31231031 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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