TMVP1448, a novel peptide improves detection of primary tumors and metastases by specifically targeting VEGFR-3.

Lymphangiogenesis at primary tumor and draining lymph nodes plays a pivotal role in tumor metastasis, which has been demonstrated to be regulated by the vascular endothelial growth factor receptor 3 (VEGFR-3) pathway. However, the effect of molecular imaging peptides, which specifically bind VEGFR-3, in tracing tumors remains unclear. We prepared a novel peptide, TMVP1448, with high-affinity to VEGFR-3. The dissociation constant (KD) of TMVP1448 with VEGFR-3 was 7.07 ×10-7 M. In vitro cellular assay showed that TMVP1448 could bind specifically with VEGFR-3. Near infrared imaging results showed that Cy7-TMVP1448 was able to accurately trace primary and metastatic cancers, and PET/CT results showed that [68Ga]Ga-DOTA-TMVP1448 was superior to commonly used radiotracers 18F-FDG. Additionally, no significant negative effect of TMVP1448 was found in mice. Our results suggested that TMVP1448 had great potential for future clinical applications in fluorescence imaging and nuclear imaging of tumors. Copyright © 2024. Published by Elsevier Masson SAS.

Citation

Yuan Yuan, Xiyuan Dong, Yuxin Chen, Ling Xi, Ding Ma, Jun Dai, Fei Li. TMVP1448, a novel peptide improves detection of primary tumors and metastases by specifically targeting VEGFR-3. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2024 Aug;177:116980

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PMID: 38908201

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