Comparison of Al18F- and 68Ga-labeled NOTA-PEG4-LLP2A for PET imaging of very late antigen-4 in melanoma
| Autor: | Huiling Li, Xiaoli Lan, Dexing Zeng, Lujie Yuan, Mengting Li, Yongkang Gai, Bouhari Altine, Lingyi Sun, Qingyao Liu, Yongxue Zhang, Hanyi Fang |
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| Rok vydání: | 2019 |
| Předmět: |
Fluorine Radioisotopes
Skin Neoplasms Peptidomimetic Gallium Radioisotopes Peptide Integrin alpha4beta1 010402 general chemistry 01 natural sciences Biochemistry Article Polyethylene Glycols Inorganic Chemistry Heterocyclic Compounds 1-Ring Mice Antigen In vivo medicine Animals Humans Melanoma chemistry.chemical_classification 010405 organic chemistry Chemistry Phenylurea Compounds VLA-4 Dipeptides Ligand (biochemistry) medicine.disease Xenograft Model Antitumor Assays In vitro 0104 chemical sciences Positron-Emission Tomography Cancer research |
| Zdroj: | J Biol Inorg Chem |
| ISSN: | 1432-1327 0949-8257 |
| Popis: | Malignant melanoma is an aggressive cancer with poor prognosis. Very late antigen-4 (VLA-4) is overexpressed in melanoma and many other tumors, making it an attractive target for developing molecular diagnostic and therapeutic agents. We compared Al(18)F- and (68)Ga-labeled LLP2A peptides for PET imaging of VLA-4 expression in melanoma. The peptidomimetic ligand LLP2A was modified with chelator 2-S-(4-isothiocyanatobenzyl)-1,4,7-triazacyclononane-1,4,7-triacetic acid (p-SCN-Bn-NOTA), and the resulting NOTA-PEG(4)-LLP2A peptide was then radiolabeled with Al(18)F or (68)Ga. The two labeled peptides were assayed for in vitro and in vivo VLA-4 targeting efficiency. Good Al(18)F and (68)Ga radiolabeling yields were achieved, and the resulting PET tracers showed good serum stability. In the in vivo evaluation of the B16F10 xenograft mouse model, both tracers exhibited high accumulation with good contrast in static PET images. Compared with (68)Ga-NOTA-PEG(4)-LLP2A, Al(18)F-NOTA-PEG(4)-LLP2A resulted in relatively higher background, including higher liver uptake (1 h: 20.1 ± 2.6 vs. 15.3 ± 1.7 %ID/g, P < 0.05; 2 h: 11.0 ± 1.2 vs. 8.0 ± 0.8 %ID/g, P < 0.05) and lower tumor-to-blood ratios (2.5 ± 0.4 vs 3.3 ± 0.5 at 1 h, P |
| Databáze: | OpenAIRE |
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