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

被引：3
作者：
Liu, Liqin [1 ]
Xu, Jingli [2 ]
Yang, Jianquan [2 ]
Feng, Changjian [3 ]
Miao, Yubin [2 ]
机构：
[1] Univ Sci & Technol Beijing, Sch Chem & Biol Engn, Beijing 100083, Peoples R China
[2] Univ Colorado Denver, Dept Radiol, Aurora, CO 80045 USA
[3] Univ New Mexico, Coll Pharm, Albuquerque, NM 87131 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 22期
关键词：
Alpha-melanocyte stimulating hormone; Tc-99m-labeled lactam-cyclized peptide; Metastatic melanoma imaging; STIMULATING HORMONE; TARGETING PROPERTIES; BRAF; VEMURAFENIB; SURVIVAL; RECEPTORS; ANALOGS;
D O I：
10.1016/j.bmcl.2017.10.022
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (C) 2017 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4952 / 4955
页数：4
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