A novel tetrapeptide for chelator-free radiolabeling in optimized preparation of 99mTc-radiolabeled oligonucleotides

被引:0
作者
Chen, Zhao [1 ]
Yang, Qi [1 ]
Song, Lele [1 ]
Qiu, Yongkang [1 ]
Wu, Sitong [2 ]
Huang, Wenpeng [1 ]
Jiang, Qiao [1 ]
Wu, Shengnan [1 ]
Kang, Lei [1 ]
机构
[1] Peking Univ, Dept Nucl Med, Hosp 1, Beijing 100034, Peoples R China
[2] Peking Univ, Dept Intervent Radiol & Vasc Surg, Hosp 1, Beijing 100034, Peoples R China
来源
AMERICAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING | 2022年 / 12卷 / 05期
关键词
Peptide; glycine-alanine-glycine-lysine; (Gly-Ala-Gly-Lys; GAGK); Tc-99m; radiolabel; anti-miRNA oligonucle-otides (AMOs); PEPTIDE NUCLEIC-ACID; ANTISENSE OLIGONUCLEOTIDES; MESSENGER-RNA; BIOLOGICAL EVALUATION; IN-VITRO; DELIVERY; TC-99M; TARGETS; MICRORNAS; CELLS;
D O I
暂无
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
Antisense imaging uses radionuclide labeled antisense oligonucleotides to hybridize with nucleic acids in vivo, display the expression of target genes, and directly quantify biological processes at the cellular and subcellular levels. The anti-miRNA oligonucleotides (AMOs) are a series of single-stranded DNA oligonucleotides that are widely used in gene imaging and gene therapy. However, due to the negative charge and high molecular weight, the permeability through the membrane of AMOs is generally low so that most AMOs cannot enter the cells. Based on the 99mTc-labeled AMOs imaging in previous studies, this study developed a novel tetrapeptide Glycine-Alanine-Glycine-Lysine (Gly-Ala-Gly-Lys, GAGK) for one-step labeling AMO with 99mTc. The labeling conditions were optimized by changing the number of stannous ions, the reaction time, and the temperature, respectively. The labeled prod-ucts were identified by gel electrophoresis and their serum stability was evaluated. The optimal labeling condition in this study was using 1 mg/mL SnCl(2)middot2H(2)O and heating for 30 min at 100 degrees C. Gel electrophoresis confirmed the verification of successful labeling of 99mTc-GAGK-AMO. After being incubated with human fresh serum for 12 h, Tc-99m-GAGK-AMO showed good stability and no obvious degradation. Therefore, this labeling method has high labeling efficiency and stable labeling, which provides an effective method for the application of miRNA-targeted imaging.
引用
收藏
页码:143 / 151
页数:9
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