2. Academic Validation
  3. In Silico Design and Evaluation of Novel Peptide-Based PET Probe for Noninvasive Imaging of HER2 Expression in Breast Cancer

In Silico Design and Evaluation of Novel Peptide-Based PET Probe for Noninvasive Imaging of HER2 Expression in Breast Cancer

  • J Med Chem. 2025 May 22;68(10):10461-10472. doi: 10.1021/acs.jmedchem.5c00760.
Xu Guo 1 2,  Chunwei Xu 3,  Xue Zhu 1 4,  Xiaojia Wang 5,  Yue Hao 6,  Xun Wang 7,  Ying Yao 2,  Jing Fang 1 4,  Ke Wang 1 4
Affiliations

Affiliations

  • 1 NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, Jiangsu 214063, China.
  • 2 Department of Pharmacy, Affiliated Women's Hospital of Jiangnan University, Wuxi Maternity and Child Health Care Hospital, Wuxi, Jiangsu 214002, China.
  • 3 Institute of Cancer and Basic Medicine (ICBM), Chinese Academy of Sciences, Hangzhou, Zhejiang 310022, China.
  • 4 Department of Radiopharmaceuticals, School of Pharmacy, Nanjing Medical University, Nanjing 211166, China.
  • 5 Department of Breast Medical Oncoloy, Zhejiang Cancer Hospital, Hangzhou, Zhejiang 310022, China.
  • 6 Department of Respiratory Medicine, Affiliated Jinling Hospital, Medical School of Nanjing University, Nanjing, Jiangsu 210002, China.
  • 7 Department of Respiratory and Critical Care Medicine, Affiliated Hospital of Jiangnan University, Wuxi, Jiangsu 214062, China.
PMID: 40322890 DOI: 10.1021/acs.jmedchem.5c00760
Abstract

The overexpression of HER2 has been strongly correlated with the pathogenesis and progression of breast Cancer. Developing HER2-targeted PET tracers for noninvasive assessment of HER2 expression holds substantial clinical significance for screening patients suitable for HER2-targeted therapy, evaluating treatment efforts, and optimizing treatment. In this study, we employed computational simulation methods to develop peptide WC8 derived from trastuzumab, and designed HER2 targeting radiotracers [68Ga]Ga-DOTA-WC8 for detecting the HER2 expression. The radiotracer demonstrated nanomolar affinity, high specificity, and favorable pharmacokinetics. PET imaging revealed that [68Ga]Ga-DOTA-WC8 exhibited significant and specific uptake in HER2-positive breast Cancer tissues, facilitating the rapid and accurate identification of HER2 expression. Notably, this radiotracer was successfully utilized to achieve direct visualization of tumor response to pyrotinib, a HER2 tyrosine kinase inhibitor. These findings suggest that the peptide-based radiotracer [68Ga]Ga-DOTA-WC8 represents a promising tool for accurately monitoring of HER2 expression after treatment with HER2-targeting drugs.

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