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An NIR‐Fluorophore‐Based Therapeutic Endoplasmic Reticulum Stress Inducer
Author(s) -
Wang Yang,
Luo Shenglin,
Zhang Chi,
Liao Xingyun,
Liu Tao,
Jiang Zhongyong,
Liu Dengqun,
Tan Xu,
Long Lei,
Wang Yu,
Chen Zelin,
Liu Yunsheng,
Yang Fan,
Gan Yibo,
Shi Chunmeng
Publication year - 2018
Publication title -
advanced materials
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 10.707
H-Index - 527
eISSN - 1521-4095
pISSN - 0935-9648
DOI - 10.1002/adma.201800475
Subject(s) - unfolded protein response , endoplasmic reticulum , fluorophore , cancer cell , cancer research , microbiology and biotechnology , mitochondrion , cancer , materials science , biophysics , biology , medicine , fluorescence , physics , quantum mechanics
The endoplasmic reticulum (ER) stress signaling or unfolded protein response (UPR) is a common feature of many human diseases, including cancer. Excessive activation of ER stress directly induces cell death, holding a new promising strategy for the therapeutic intervention of cancer. Current ER‐stress‐inducing agents mainly target UPR components or proteasomes, which exert limited treatment efficacy and undesired side effects due to unselective ER stress and poor tumor‐specific distribution. In this study, a unique near‐infrared (NIR) fluorophore, IR‐34, is synthesized and identified to selectively and efficiently trigger tumoricidal ER stress by targeting the mitochondrial protein NDUFS1. IR‐34 is demonstrated to specifically accumulate in living cancer cells for tumor NIR imaging and drastically inhibit tumor growth and recurrence without causing apparent toxicity. Thus, this multifunctional NIR fluorophore may represent a novel theranostic agent for tumor imaging‐guided treatment and also strengthens the idea that mitochondria could be a useful target for therapeutic ER stress in cancer cells.