吡啶
四苯乙烯
自噬
粒体自噬
线粒体
溶酶体
自噬体
化学
体内
癌细胞
烷基
荧光
材料科学
癌症
细胞生物学
聚集诱导发射
有机化学
生物化学
医学
生物
细胞凋亡
酶
生物技术
内科学
物理
量子力学
作者
Yanyan Huang,Xu You,Lingna Wang,Guanxin Zhang,Shilang Gui,Yulong Jin,Rui Zhao,Deqing Zhang
标识
DOI:10.1002/anie.202001906
摘要
Abstract Tuning autophagy in a controlled manner could facilitate cancer therapy but it remains challenging. Pyridinium‐substituted tetraphenylethylene salts (PTPE 1 — 3 ), able to target mitochondria and disrupt autophagy after forming complexes with albumin, are reported. Mitochondrion affinity and autophagy‐inducing activity are improved by prolonging the length of alkyl chains in PTPE 1 – 3 . PTPE 1 – 3 demonstrate proautophagic activity and a mitophagy blockage effect. Failure of autophagosome–lysosome fusion in downstream autophagy flux results in cancer cell death. Moreover, fast formation of complexes of PTPE 1 – 3 with albumin in blood can facilitate biomimetic delivery and deep tumor penetration. Efficient tumor accumulation and effective tumor suppression are successfully demonstrated with in vitro and in vivo studies. PTPE 1 – 3 salts exhibit dual functionality: they target and image mitochondria because of aggregation‐induced emission effects and they are promising for cancer therapy.
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