2. Academic Validation
  3. PET Imaging of Solid Tumors with a G-Quadruplex-Targeting 18F-Labeled Peptide Probe

PET Imaging of Solid Tumors with a G-Quadruplex-Targeting 18F-Labeled Peptide Probe

  • J Med Chem. 2025 Feb 13;68(3):2804-2814. doi: 10.1021/acs.jmedchem.4c02121.
Xiao-Chun Guo 1,  Da-Zhi Shi 2,  Shun Huang 3,  Yi-Han Zhang 1,  Wan-Ying Zhang 1,  Jing Chen 1,  Zebin Huang 1,  Hubing Wu 2,  Jin-Qiang Hou 4 5,  Fu-Jun Jin 1,  Xiu-Cai Chen 1,  Wing-Leung Wong 6,  Yu-Jing Lu 1 7
Affiliations

Affiliations

  • 1 Guangdong Medicine-Engineering Interdisciplinary Technology Research Center, School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, China.
  • 2 Department of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China.
  • 3 Department of Nuclear Medicine, The Tenth Affiliated Hospital, Southern Medical University (Dongguan People's Hospital), Dongguan 523059, China.
  • 4 Department of Chemistry, Lakehead University, 955 Oliver Road, Thunder Bay, Ontario P7B 5E1, Canada.
  • 5 Thunder Bay Regional Health Research Institute, 980 Oliver Road, Thunder Bay, Ontario P7B 6 V4, Canada.
  • 6 State Key Laboratory of Chemical Biology and Drug Discovery, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong SAR 999077, China.
  • 7 Smart Medical Innovation Technology Center, Guangdong University of Technology, Guangzhou 510006, China.
PMID: 39807685 DOI: 10.1021/acs.jmedchem.4c02121
Abstract

Positron emission tomography (PET) is a common imaging technique and can provide accurate information about the size, shape, and location of tumors. Recent evidence has shown that G-quadruplex structures (G4s) are identified in human oncogenes, and these special structures are recognized as diagnostic Cancer markers and drug targets for Anticancer therapies. Although a number of techniques for in vivo imaging of G4s have been developed, achieving sufficient sensitivity and selectivity in vivo remains challenging. Herein, we have engineered and developed a radiolabeled peptide probe [18F]AlF-NOTA-RHAU18 targeting mitochondrial DNA G4s for in vivo PET imaging. The results of the study indicate that this probe is able to visualize and detect solid tumors in living homozygous mice. In addition, the distribution of the probe in Cancer cells was investigated using FITC-RHAU18. This work may offer new insights into the development of Cancer diagnostic tools by targeting in vivo G4s.

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