Lysosome-Instructed Self-Assembly of Amino-Acid-Functionalized Perylene Diimide for Multidrug-Resistant Cancer Cells

Changjoon Keum, Jiyoung Hong, Doyeon Kim, Sang Yup Lee, Hyuncheol Kim

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)


Multidrug resistance (MDR) of cancer cells reduces chemotherapeutic efficacy by preventing drug accumulation in the cells through a drug efflux pump and lysosomal sequestration/exocytosis. Herein, to overcome such anticancer resistance, lysosome-targeted self-assembly of perylene diimide (PDI) derivatives is presented as a powerful strategy for effective and selective anticancer therapy. Stimulated by the lysosomal low pH, the amphiphilic PDI derivatives functionalized with amino acids (PDI-AAs) construct fibrous self-assembled structures inside the lysosomes, causing cancer cell apoptosis by lysosomal rupture. In contrast, negligible apoptosis was observed from normal cells by PDI-AA. The agglomerated fibrous assemblies were not removed by lysosomal exocytosis, thereby displaying a 10.7-fold higher anticancer efficacy on MDR cancer cells compared to a doxorubicin chemotherapeutic agent. The MDR-circumventing capability, along with high selectivity toward cancer cells, supports PDI-AAs as potential candidates for the treatment of MDR cancer cells by lysosome-targeted self-assembly.

Original languageEnglish
Pages (from-to)14866-14874
Number of pages9
JournalACS Applied Materials and Interfaces
Issue number13
Publication statusPublished - 2021 Apr 7

Bibliographical note

Funding Information:
This study was supported by a grant from the Korean Research Foundation funded by the Korean Government (NRF-2019R1A2C1010629 and NRF- 2020R1A2B5B02001733).

Publisher Copyright:

All Science Journal Classification (ASJC) codes

  • Materials Science(all)


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