“Click” synthesis of small molecule–peptide conjugates for organelle-specific delivery and inhibition of lysosomal cysteine proteases

Abstract

A click chemistry approach for the synthesis of small molecule inhibitor–peptide conjugates to achieve organelle-specific delivery has been developed. Biological testing showed that the inhibitor–Tat conjugate was successfully delivered to the lysosomes, leading to potent inhibition of lysosomal cysteine proteases in cultured cells.