4.7 Article

Hypoxia-Responsive Luminescent CEST MRI Agent forIn VitroandInVivoTumor Detection and Imaging

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 65, Issue 10, Pages 7106-7117

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.1c01745

Keywords

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Funding

  1. National Research Council of Science and Technology (NST) grant from the Korea government (MSIT) [CAP-18-02-KRIBB]
  2. National Research Foundation of Korea (NRF) - Korea government (MSIT) [2020R1A2C2012011]
  3. Korea Basic Science Institute [C130000]
  4. Robert A. Welch Foundation [F-0018]
  5. National Research Council of Science & Technology (NST), Republic of Korea [C130000] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
  6. National Research Foundation of Korea [2020R1A2C2012011] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)

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A bimodal probe based on molecular antenna was developed for enhanced imaging of solid tumors under hypoxic conditions. The probe exhibited both magnetic resonance and optical signals, allowing for improved tumor detection and monitoring.
Hypoxia is a feature of most solid tumors and a keydeterminant of cancer growth and propagation. Sensing hypoxiaeffectively could lead to more favorable clinical outcomes. Here, wereport a molecular antenna-based bimodal probe designed toexploit the complementary advantages of magnetic resonance(MR)- and optical-based imaging. Specifically, we describe thesynthesis and evaluation of a dual-action probe (NO2-Eu) thatpermits hypoxia-activated chemical exchange saturation transfer(CEST) MR and optical imaging. In CT26 cells, thisNO2-Euprobe not only provides an enhanced CEST MRI signal but alsoturnsonthe optical signal under hypoxic conditions. Time-dependentin vivoCEST imaging in a hypoxic CT26 tumorxenograft mouse model revealed probe-dependent tumor detectionby CEST MRI contrast in the tumor area. We thus suggest that dual-action hypoxia probes, like that reported here, could have a roleto play in solid tumor diagnosis and monitoring

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