Synthesis of a novel 99m Tc labeled GE11 peptide for EGFR SPECT imaging
This study investigated a novel SPECT agent for the noninvasive imaging of EGFR-overexpressing tumors. 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 Tc. The radiochemical yield of...
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Published in | International journal of radiation biology Vol. 96; no. 11; pp. 1443 - 1451 |
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Main Authors | , , , , |
Format | Journal Article |
Language | English |
Published |
England
01.11.2020
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Subjects | |
Online Access | Get full text |
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Summary: | This study investigated a novel SPECT agent for the noninvasive imaging of EGFR-overexpressing tumors.
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
Tc. The radiochemical yield of the
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.
The
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
Tc-peptide-GE11 in A549 xenograft than in H23 xenografts.
The new SPECT tracer
c-peptide-GE11 showed EGFR specificity, favorable pharmacokinetics and great potential for EGFR-targeted imaging. |
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ISSN: | 0955-3002 1362-3095 |
DOI: | 10.1080/09553002.2020.1811419 |