Intracellular aggregation of peptide-reprogrammed small molecule nanoassemblies enhances cancer chemotherapy and combinatorial immunotherapy.

Author: Jinrong PENG ¹ ; Yao XIAO ¹ ; Qian YANG ¹ ; Qingya LIU ¹ ; Yu CHEN ¹ ; Kun SHI ¹ ; Ying HAO ¹ ; Ruxia HAN ¹ ; Zhiyong QIAN ¹
Author Information

1. State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, And Collaborative Innovation Center of Biotherapy, Chengdu 610065, China.
Publication Type:Journal Article
Keywords: Chemotherapy; Combinational immunotherapy; Glutathione response; Intracellular aggregation; Nanoassembly
From: Acta Pharmaceutica Sinica B 2021;11(4):1069-1082
CountryChina
Language:English
Abstract: The intracellular retention of nanotherapeutics is essential for their therapeutic activity. The immobilization of nanotherapeutics inside target cell types can regulate various cell behaviors. However, strategies for the intracellular immobilization of nanoparticles are limited. Herein, a cisplatin prodrug was synthesized and utilized as a glutathione (GSH)-activated linker to induce aggregation of the cisplatin prodrug/IR820/docetaxel nanoassembly. The nanoassembly has been reprogrammed with peptide-containing moieties for tumor-targeting and PD-1/PD-L1 blockade. The aggregation of the nanoassemblies is dependent on GSH concentration. Evaluations