Intracellular delivery of therapeutic proteins through N-terminal site-specific modification.

A versatile strategy for the intracellular delivery of functional proteins/antibodies was developed using N-terminal site-specific modification. Adopting orthogonal dual-labeling strategies, a cell-permeable RNase A prodrug was designed complementing N-terminal site-specific modification with lysine labeling. Upon successful cytosolic uptake, the prodrug showed reactive oxygen species (ROS)-dependent targeted cancer therapy.