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Related Experiment Video

Updated: Jul 2, 2026

Radionuclide-fluorescence Reporter Gene Imaging to Track Tumor Progression in Rodent Tumor Models
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Published on: March 13, 2018

Drug Screening of Nitroreductase Modulators Using an Atomic-Engineered Activatable Fluorescent Probe for Tumor

Fei Han1, Suntao Shi1, Liangying Mi1

  • 1State Key Laboratory of Natural Product Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, China.

Journal of Medicinal Chemistry
|July 1, 2026
PubMed
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This summary is machine-generated.

Researchers developed novel nitroreductase (NTR)-activated fluorescent probes for precise tumor imaging. These probes aid in distinguishing cancer cells and show potential for intraoperative navigation and drug screening.

Area of Science:

  • Biomedical Engineering
  • Chemical Biology
  • Molecular Imaging

Background:

  • Nitroreductase (NTR) is a hypoxia-upregulated enzyme and a potential biomarker for solid tumors.
  • Effective biosensors are needed for NTR detection, driving interest in fluorescent probes.
  • Cyanine dyes are versatile fluorophores used in various biomedical applications.

Purpose of the Study:

  • To design and synthesize novel NTR-activated fluorescent probes using atomic engineering.
  • To evaluate the lead probe (HCy-NS-4) for its optical properties and imaging capabilities.
  • To explore the potential of the probe in intraoperative tumor navigation and drug screening.

Main Methods:

  • Atomic engineering via heteroatom substitution (C, O, S) to design four NTR-activated probes.

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  • Optical characterization of probes, including fluorescence enhancement and emission wavelength.
  • In vitro and in vivo studies for imaging hypoxic NTR, distinguishing cell types, and assessing tumor navigation.
  • Main Results:

    • HCy-NS-4 was identified as the lead probe with near-infrared emission (712 nm) and >18-fold fluorescence enhancement.
    • The probe enabled precise imaging of hypoxic NTR and differentiation of malignant from nonmalignant cells.
    • Luteolin was identified as an NTR modulator with antitumor activity, using HCy-NS-4 as a screening tool.

    Conclusions:

    • The developed NTR-activated probes are effective tools for precise tumor imaging and intraoperative navigation.
    • HCy-NS-4 demonstrates significant potential for distinguishing tumor tissues and guiding surgical procedures.
    • This study presents a novel model for drug screening by combining molecular design with inhibitor discovery.