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Title: Novel dual-function near-infrared II fluorescence and PET probe for tumor delineation and image-guided surgery

Journal Article · · Chemical Science
DOI:https://doi.org/10.1039/C7SC04774F· OSTI ID:1417921
 [1];  [1];  [1];  [2];  [2];  [1];  [1];  [3];  [3];  [4];  [4];  [5];  [5];  [1];  [2]; ORCiD logo [1]
  1. State Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) and Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China
  2. Molecular Imaging Program at Stanford (MIPS), Bio-X Program, Department of Radiology, Stanford University, USA
  3. Medical College, Tibet University, Lasa, China
  4. Hubei Provincial Key Laboratory of Developmentally Originated Disease, Center for Experimental Basic Medical Education, Wuhan University, Wuhan 430071, China
  5. Department of Nuclear Medicine, The Second Hospital of Zhejiang University School of Medicine, Hangzhou, China

Accurate tumor identification is essential in cancer management. Incomplete excision of tumor tissue, however, negatively affects the prognosis of the patient. To accomplish radical excision of tumor tissue, radiotracers can be used that target tumor tissue and can be detected using a gamma probe during surgery. Intraoperative fluorescence imaging could allow accurate real-time tumor delineation. Herein, a novel dual-modal imaging platform using base-catalyzed double addition of thiols into a propiolamide scaffold has been developed, allowing for the highly efficient and selective assembly of various thiol units in a protecting-group-free manner. The first small-molecule based αvβ3-targeted NIR-II/PET probe 68Ga-SCH2 was concisely generated via this strategy and subsequently evaluated in mice bearing the U87MG xenograft. Excellent imaging properties such as good tumor uptake, high tumor contrast and specificity, tumor delineation and image-guided surgery were achieved in the small animal models. These attractive results of 68Ga-SCH2 allow it to be a promising αvβ3-targeted NIR-II/PET probe for clinical translation.

Research Organization:
Stanford Univ., CA (United States)
Sponsoring Organization:
USDOE Office of Science (SC), Biological and Environmental Research (BER)
Grant/Contract Number:
SC0008397
OSTI ID:
1417921
Alternate ID(s):
OSTI ID: 1506079
Journal Information:
Chemical Science, Journal Name: Chemical Science Vol. 9 Journal Issue: 8; ISSN 2041-6520
Publisher:
Royal Society of Chemistry (RSC)Copyright Statement
Country of Publication:
United Kingdom
Language:
English
Citation Metrics:
Cited by: 135 works
Citation information provided by
Web of Science

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