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Synthesis of a novel(99m)Tc labeled GE11 peptide for EGFR SPECT imaging

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机构: [1]Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang 050011, China [2]Department of Neurology, The Second Hospital of Hebei Medical University, Shijiazhuang 050011, China
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关键词: EGFR NSCLC SPECT radionuclide imaging Tc-99m-labeled peptide conjugates

摘要:
Purpose This study investigated a novel SPECT agent for the noninvasive imaging of EGFR-overexpressing tumors. Methods The EGFR-targeting peptide GE11 was synthesized with the introduction of four amino acids (GGGC) to its C-terminal to act as a strong chelator and radiolabeled using(99m)Tc. The radiochemical yield of the(99m)Tc-peptide-GE11 were evaluated using RP-HPLC. Cellular assays of the probe were performed on two NSCLC cell lines: A549 (high expression) and H23 (low expression). Biodistribution and SPECT imaging were performed in BALB/c nude mice bearing A549 and H23 NSCLC xenografts. Results The(99m)Tc-peptide-GE11 was prepared at high efficiency with radiochemical yield of 98.40 +/- 1.00 % and it showed favorable stability. The cellular uptake was significantly higher in A549 than in H23 at all time points (especially at 1 h, which was 10.34 +/- 0.72 and 2.04 +/- 0.18, respectively). A nearly 56% reduction in probe uptake was observed after pretreatment with excess unlabeled peptides. The performance of SPECT imaging and biodistribution demonstrated higher uptake of the(99m)Tc-peptide-GE11 in A549 xenograft than in H23 xenografts. Conclusion The new SPECT tracer(99mT)c-peptide-GE11 showed EGFR specificity, favorable pharmacokinetics and great potential for EGFR-targeted imaging.

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出版当年[2020]版:
大类 | 4 区 医学
小类 | 2 区 核科学技术 3 区 生物学 4 区 核医学
最新[2025]版:
大类 | 4 区 医学
小类 | 3 区 核科学技术 4 区 生物学 4 区 核医学
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出版当年[2020]版:
Q1 NUCLEAR SCIENCE & TECHNOLOGY Q2 BIOLOGY Q3 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING
最新[2024]版:
Q1 NUCLEAR SCIENCE & TECHNOLOGY Q2 BIOLOGY Q2 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING

影响因子: 最新[2024版] 最新五年平均 出版当年[2020版] 出版当年五年平均 出版前一年[2019版] 出版后一年[2021版]

第一作者:
第一作者机构: [1]Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang 050011, China [2]Department of Neurology, The Second Hospital of Hebei Medical University, Shijiazhuang 050011, China
通讯作者:
通讯机构: [1]Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, Shijiazhuang 050011, China [*1]Department of Nuclear Medicine, The Fourth Hospital of Hebei Medical University, JianKang Road, Shijiazhuang, 050011, P. R. China.
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