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

Authors: Loh, Yuhui; Shi, Haibin; Hu, Mingyu; Yao, Shao Q.; Chemical Communications; (2010); 10.1039/c0cc03738a

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.