Many bioconjugation strategies for DNAo ligonucleotides and antibodies suffer limitations,s uch as sitespecificity,s toichiometry and hydrolytic instability of the conjugates,w hichm akes them unsuitable for biological applications.H ere,w er eport an ew platform for the preparation of DNA-antibody bioconjugates with as imple benzoylacrylic acid pentafluorophenyl ester reagent. Benzoylacryliclabelled oligonucleotides prepared with this reagent can be sitespecifically conjugated to ar ange of proteins and antibodies through accessible cysteine residues.T he homogeneity of the prepared DNA-antibody bioconjugates was confirmed by an ew LC-MS protocol and the bioconjugate probes were used in fluorescence or super-resolution microscopyc ell imaging experiments.T his work demonstrates the versatility and robustness of our bioconjugation protocol that gives sitespecific,w ell-defined and plasma-stable DNA-antibody bioconjugates for biological applications.

Owing to their bioorthogonality, transition metals have become very popular in the development of biocompatible bond‐cleavage reactions. However, many approaches require design and synthesis of complex ligands or formulation of nanoparticles which often perform poorly in living cells. This work reports on a method for the generation of an active palladium species that triggers bond‐cleaving reactions inside living cells. We utilized the water‐soluble Na2PdCl4 as a simple source of PdII which can be intracellularly reduced by sodium ascorbate to the active Pd0 species. Once generated, Pd0 triggers the cleavage of allyl ether and carbamate caging groups leading to the release of biologically active molecules. These findings do not only expand the toolbox of available bioorthogonal dissociative reactions but also provide an additional strategy for controlling the reactivity of Pd species involved in Pd‐mediated bioorthogonal reactions.

Owing to their bioorthogonality, transition metals have become very popular in the development of biocompatible bond-cleavage reactions. However, many approaches require design and synthesis of complex ligands or formulation of nanoparticles which often perform poorly in living cells. This work reports on a method for the generation of an active palladium species that triggers bond-cleaving reactions inside living cells. We utilized the water-soluble Na 2 PdCl 4 as a simple source of Pd II which can be intracellularly reduced by sodium ascorbate to the active Pd 0 species. Once generated, Pd 0 triggers the cleavage of allyl ether and carbamate caging groups leading to the release of biologically active molecules. These findings do not only expand the toolbox of available bioorthogonal dissociative reactions but also provide an additional strategy for controlling the reactivity of Pd species involved in Pd-mediated bioorthogonal reactions.

Sugar-modified pyrimido[4,5-b]indole nucleosides (2′-deoxy-2′-fluororibo-, 2′-deoxy-2′-fluoroarabino- and arabinonucleosides) were found to be low micromolar antivirals against HCV or dengue.