Palladium-Mediated Incorporation of Carboranes into Small Molecules, Peptides, and Proteins.

ABSTRACT: Carboranes represent a class of compounds with increasing therapeutic potential. However, few general approaches to readily embed carboranes into small molecules, peptides, and proteins are available. We report a strategy based on palladium-mediated C-X (X = C, S, and N) bond formation for the installation of carborane-containing moieties onto small molecules and peptides. We demonstrate the ability of Pd-based reagents with appropriate ligands to overcome the high hydrophobicity of the carborane group and enable chemoselective conjugation of cysteine residues at room temperature in aqueous buffer. Accordingly, carboranes can be efficiently installed on proteins by employing a combination of a bis-sulfonated biarylphosphine-ligated Pd reagent in an aqueous histidine buffer. This method is

SUBMITTER: Gazvoda M 

PROVIDER: S-EPMC9881053 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature