Facile preparation of a novel Ga-67-labeled NODAGA-conjugated lactam-cyclized alpha-MSH peptide at room temperature for melanoma targeting.
Facile preparation of a novel Ga-67-labeled NODAGA-conjugated lactam-cyclized alpha-MSH peptide at room temperature for melanoma targeting.
复制标题
DOI：
10.1016/j.bmcl.2020.127627
复制
发表时间：
2020-12-15
影响因子：
2.7
通讯作者：
Miao Y
中科院分区：
文献类型：
--
作者：
Xu J;Qiao Z;Gonzalez R;Miao Y
本研究测定了67Ga-NODAGA-GGNLE-CycMSHhex(1，4，7-三氮杂环酮，1-谷氨酸-4，7-乙酸酯acid-GlyGlyNle-c[Asp-His-dPhe-Arg-Trp-Lys]-CONH2})在荷B16/F10黑色素瘤C57小鼠体内的靶向性，以论证NODAGA作为放射性金属螯合剂用于室温放射性标记NODAGA-GGNLE-CycMSHhex的可行性。NODAGA-GGNle-CycMSHhex对B16/F10黑色素瘤细胞的IC50值为0.87±0.12 nM。67Ga-NODAGA-GGNle-CycMSHhex在室温下制备容易，放射性标记率大于98%，并与B16/F10黑色素瘤细胞显示MC1R特异性结合。注射后0.5、2、4和24 h，67Ga-NODAGA-GGNle-CycMSHhex对B16/F10黑色素瘤的摄取分别为10.31±0.78、14.96±1.34、13.7±3.33和10.4±2.2%ID/g。大约85%的注射剂量在注射后2小时通过泌尿系统清除。67Ga-NODAGA-GGNle-CycMSHhex注射后2 h，肿瘤/血液、肿瘤/肌肉、肿瘤/皮肤摄取比值均较高。总体而言，67Ga-NODAGA-GGNLE-CycMSHhex可以在室温下轻松制备，并表现出良好的黑色素瘤靶向性，提示NODAGA作为放射性金属螯合剂用于α-MSH多肽的室温放射性标记具有潜在的应用前景。
In this study, the melanoma targeting property of 67Ga-NODAGA-GGNle-CycMSHhex {1,4,7-triazacyclononane,1-gluteric acid-4,7-acetic acid-GlyGlyNle-c[Asp-His-dPhe-Arg-Trp-Lys]-CONH2} was determined on B16/F10 melanoma-bearing C57 mice to demonstrate the feasibility of NODAGA as a radiometal chelator for facile room temperature radiolabeling of NODAGA-GGNle-CycMSHhex. The IC50 value of NODAGA-GGNle-CycMSHhex was 0.87 ± 0.12 nM on B16/F10 melanoma cells. 67Ga-NODAGA-GGNle-CycMSHhex was readily prepared at room temperature with greater than 98% radiolabeling yield and displayed MC1R-specific binding on B16/F10 melanoma cells. The B16/F10 melanoma uptake of 67Ga-NODAGA-GGNle-CycMSHhex was 10.31 ± 0.78, 14.96 ± 1.34, 13.7 ± 3.33 and 10.4 ± 2.2% ID/g at 0.5, 2, 4 and 24 h post-injection, respectively. Approximately 85% of injected dose cleared out the body via urinary system at 2 h post-injection. 67Ga-NODAGA-GGNle-CycMSHhex showed high tumor/blood, tumor/muscle and tumor/skin uptake ratios after 2 h post-injection. Overall, 67Ga-NODAGA-GGNle-CycMSHhex could be easily prepared at room temperature and exhibited favorable melanoma targeting property, suggesting the potential use of NODAGA as a radiometal chelator for facile room temperature radiolabeling of α-MSH peptides.
登录
查看更多内容
影响因子：
3.4
作者：
Xu, Jingli;Yang, Jianquan;Miao, Yubin
通讯作者：
Miao, Yubin
DOI：
10.2967/jnumed.110.086009
发表时间：
2011-04
期刊：
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子：
--
作者：
Guo H;Yang J;Gallazzi F;Miao Y
通讯作者：
Miao Y
影响因子：
17.1
作者：
Yang J;Xu J;Gonzalez R;Lindner T;Kratochwil C;Miao Y
通讯作者：
Miao Y
影响因子：
254.7
作者：
Jemal, Ahmedin;Siegel, Rebecca;Ward, Elizabeth
通讯作者：
Ward, Elizabeth
影响因子：
4.9
作者：
Guo, Haixun;Miao, Yubin
通讯作者：
Miao, Yubin