A novel ICG-labeled cyclic TMTP1 peptide dimer for sensitive tumor imaging and enhanced photothermal therapy in vivo

• DOI: 10.1016/j.ejmech.2021.113935
• Publication Date: 2021-10-21T22:21:39Z
• Authors: Ling Wang; Danya Zhang; Jie Li; Fei Li; Rui Wei; Guiying Jiang; Hanjie Xu; Xueqian Wang; Ying Zhou; Ling Xi
• Keywords: Biodistribution; Indocyanine Green

TMTP1 is a polypeptide independently screened in our laboratory, which can target tumors situ and metastases. In previous work, we have successfully developed near-infrared (NIR) probe TMTP1-PEG4-ICG for tumor imaging. However, the limited ability to micrometastases hinders its further clinical application. Multimerization of peptides has been extensively demonstrated as an effective strategy increase receptor binding affinity due "multivalent effect" or "apparent cooperative affinity". this study, novel homodimer-directed NIR (TMTP1-PEG4)2-ICG was constructed synthesized. The cyclic were bridged by two PEG4 linkers then labeled with ICG-NHS imaging photothermal therapy. vivo biodistribution assessed normal BALB/c mice, targeting abilities monomer evaluated compared 4T1-bearing subcutaneous lymph node metastasis model mice. Biodistribution analysis revealed that cleared mainly both liver kidney dependent way. Comparing free ICG dye probe, improved dimer showed more sensitive could clearly identify at minimum volume 10 mm3. Additionally, when monomer, (LN) metastases also be apparently visualized easily distinguished from LN 24 h post-injection. blocking study accumulation specifically medicated receptor-ligand interaction. Furthermore, stability vivo, attractive agent significantly inhibit growth under 808 nm laser irradiation. conclusion, work promising theranostic imaging-guided therapy, indicating broad prospects transformation.