Metastatic melanoma imaging using a novel Tc-99m-labeled lactam-cyclized alpha-MSH peptide

作者：Liu, Liqin; Xu, Jingli; Yang, Jianquan; Feng, Changjian; Miao, Yubin^*

来源：Bioorganic & Medicinal Chemistry Letters, 2017, 27(22): 4952-4955.

DOI：10.1016/j.bmcl.2017.10.022

• Alpha-melanocyte stimulating hormone
• Tc-99m-labeled lactam-cyclized peptide
• Metastatic melanoma imaging

The purpose of this study was to determine the metastatic melanoma imaging property of Tc-99m(EDDA)-HYNIC- Aoc-Nle-CycMSH(hex) {hydrazinonicotinamide-8-aminooctanoic acid-Nle-c[ Asp-His-DPhe-Arg-Trp-Lys]-CONH2}. HYNIC-Aoc-Nle-CycMSH(hex) was synthesized using fluorenylmethyloxy carbonyl (Fmoc) chemistry. The IC50 value of HYNIC-Aoc-Nle-CycMSH(hex) was 0.78 +/- 0.13 nM for B16/F10 melanoma cells. Tc-99m(EDDA)-HYNIC-Aoc-Nle-CycMSH(hex) displayed significantly higher uptake (14.26 +/- 2.74 and 10.45 +/- 2.31% ID/g) in B16/F10 metastatic melanoma-bearing lung than that in normal lung (0.90 +/- 0.15 and 0.53 +/- 0.14% ID/g) at 2 and 4 h post-injection, respectively. B16/F10 pulmonary metastatic melanoma lesions were clearly visualized by SPECT/CT using Tc-99m(EDDA)-HYNIC-Aoc-Nle-CycMSH(hex) as an imaging probe at 2 h post-injection, underscoring its potential as an imaging probe for metastatic melanoma detection.

• 出版日期2017-11-15
• 单位北京科技大学