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Related Experiment Video

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An intracellularly activatable, fluorogenic probe for cancer imaging.

Ruisong Tian1, Mingjie Li, Jin Wang

  • 1State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin 300071, P. R. China. hongzy@nankai.edu.cn.

Organic & Biomolecular Chemistry
|May 31, 2014
PubMed
Summary
This summary is machine-generated.

A novel dual-functional probe offers "turn-on" cancer cell detection. Activated by cathepsin B in cancer cells, it enhances fluorescence for improved surgical visualization.

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Area of Science:

  • Biomedical Engineering
  • Molecular Imaging
  • Cancer Diagnostics

Background:

  • Developing sensitive and specific probes for cancer cell detection is crucial for early diagnosis and effective treatment.
  • Existing "always-on" probes can suffer from high background fluorescence and non-specific enzyme activation, limiting their clinical utility.
  • Intracellular activation strategies offer a promising approach to enhance probe specificity and signal-to-noise ratio.

Purpose of the Study:

  • To design and develop a novel dual-functional probe for targeted cancer cell detection.
  • To achieve "turn-on" fluorescence visualization of cancer cells through intracellular activation.
  • To evaluate the probe's specificity, sensitivity, and potential for intraoperative cancer surgery.

Main Methods:

  • A dual-functional probe was designed with efficient Förster Resonance Energy Transfer (FRET) quenching for low background fluorescence.
  • The probe utilizes folate receptor-mediated endocytosis for selective internalization into cancer cells.
  • Probe activation was triggered by intracellular cathepsin B cleavage, leading to significant fluorescence enhancement.

Main Results:

  • The developed probe exhibited near-non-fluorescence in buffer due to efficient FRET quenching.
  • Specific activation and dramatic fluorescence enhancement were observed upon intracellular cathepsin B cleavage in target cancer cells.
  • The probe demonstrated selective internalization via folate receptor-dependent endocytosis.
  • The "turn-on" probe provided high specificity and contrast enhancement for cancer cell visualization.
  • Low fluorescence-quenched background and avoidance of non-specific enzyme activation were achieved.

Conclusions:

  • The newly designed, intracellularly activatable probe enables specific "turn-on" visualization of cancer cells.
  • This probe offers advantages over "always-on" probes by minimizing background noise and non-specific activation.
  • The probe holds significant potential for intraoperative cancer surgery, offering higher contrast and sensitivity for improved detection.