| Literature DB >> 32631560 |
Qingyu Lin1, Yingying Zhang2, Zhequan Fu2, Bingxin Hu2, Zhan Si2, Yanzhao Zhao2, Hongcheng Shi3, Dengfeng Cheng4.
Abstract
c-MET-positive NSCLC is an important subtype accounting for about 5%~22% of lung cancer. NSCLC patients with activating c-MET are intensively sensitive to c-MET selective receptor tyrosine kinase (RTK) inhibitors, so we aimed to develop a specific PET probe targeting to c-MET-positive NSCLC for potential patients screened by PET/CT. Herein, PET tracer 18F-radiolabeled crizotinib derivative ([18F]FPC) was successfully achieved through a simple one-step 18F-labeling method. [18F]FPC PET imaging on c-MET-positive (as well as blocking group) and negative NSCLC models were further evaluated, and results showed that [18F]FPC was effective as a PET imaging probe that targeted c-MET-positive tumor. Therefore, [18F]FPC could be a potential PET imaging probe for NSCLC tumor which was sensitive to c-MET-TKIs. By virtue of this property, it will benefit NSCLC patients for c-MET-TKI treatment.Entities:
Keywords: Cellular-mesenchymal to epithelial transition factor (c-MET); Crizotinib; Non-small-cell lung carcinoma (NSCLC); Positron emission tomography (PET); [(18)F]FPC
Mesh:
Substances:
Year: 2020 PMID: 32631560 DOI: 10.1016/j.bmc.2020.115577
Source DB: PubMed Journal: Bioorg Med Chem ISSN: 0968-0896 Impact factor: 3.641