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A Phosphinate-Containing Fluorophore Capable of Selectively Inducing Apoptosis in Cancer Cells. | LitMetric

AI Article Synopsis

  • Chemotherapeutic agents often harm healthy cells, causing side effects, so researchers seek more selective compounds that target only cancer cells.
  • Our lab has created new near-infrared (NIR) fluorophores, called Nebraska Red (NR), with potential for this targeted approach.
  • One NR variant showed selective toxicity to HeLa cervical cancer cells while sparing NIH-3T3 noncancerous cells, and its effectiveness is linked to its unique location within cells based on mitochondrial activity.

Article Abstract

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 , against HeLa (cervical cancer) cells versus NIH-3T3 (noncancerous fibroblast) cells. Mechanistic studies based on the NIR fluorescence signal of NR 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.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6663559PMC
http://dx.doi.org/10.1002/cbic.201800811DOI Listing

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