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A Phosphinate‐Containing Fluorophore Capable of Selectively Inducing Apoptosis in Cancer Cells
Author(s) -
Zhou Xinqi,
Fang Yuan,
Lesiak Lauren,
Stains Cliff I.
Publication year - 2019
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201800811
Subject(s) - hela , cytotoxicity , fluorophore , cancer cell , chemistry , apoptosis , cell , biochemistry , fluorescence , microbiology and biotechnology , cancer research , cancer , biology , in vitro , physics , genetics , quantum mechanics
Chemotherapeutic agents generally suffer from off‐target cytotoxicity in noncancerous cell types, leading to undesired side effects. As a result, significant effort has been put into identifying compounds that are selective for cancerous over noncancerous cell types. Our laboratory has recently developed a series of near‐infrared (NIR) fluorophores containing a phosphinate functionality at the bridging position of a xanthene scaffold, termed Nebraska Red (NR) fluorophores. Herein, we report the selective cytotoxicity of one NR derivative, NR 744 , against HeLa (cervical cancer) cells versus NIH‐3T3 (noncancerous fibroblast) cells. Mechanistic studies based on the NIR fluorescence signal of NR 744 showed distinct subcellular localization in HeLa (mitochondrial) versus NIH‐3T3 (lysosomal) that resulted from the elevated mitochondrial potential in HeLa cells. This study provides a new, NIR scaffold for the further development of reagents for targeted cancer therapy.