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<p>The CLDN18.2 protein, which is highly expressed in tumors such as gastric cancer, has emerged as a critical molecular target for the development of anti-cancer diagnostic and therapeutic drugs. The CLDN18.2-targeted peptide radiopharmaceutical [<sup>131</sup>I]I-yg-15 was prepared and evaluated in this study. Molecular docking simulations reveal the binding site between the peptide and the CLDN18.2 protein at the atomic level. Under optimized preparation conditions, [<sup>131</sup>I]I-yg-15 achieved a labeling efficiency of 96.86 ± 1.34% and a specific activity of 5.63&#xa0;GBq/μmol. In CLDN18.2-overexpressing cells, cellular uptake within 1&#xa0;h was 3.31 ± 0.14%, significantly higher than that in the blocking group (1.0 ± 0.39%). SPECT-CT imaging and biodistribution studies confirmed that [<sup>131</sup>I]I-yg-15 specifically targeted and accumulated in CLDN18.2-positive tumor tissues, with a 1-h SUV of 0.41 ± 0.04, initially demonstrating the feasibility of peptide radiopharmaceuticals for the diagnosis and treatment of 18.2-positive tumors.</p>

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Preparation and preliminary biological evaluation of [131I]I-yg-15 peptide

  • 期刊论文

  • 发表日期：

    2026年3月23日

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  • Yang Wang,
  • Yuxin Wang,
  • Xuecen Cao,
  • Zijun Kuang,
  • Lin Ma,
  • Lan Zhang,
  • Yuxia Liu,
  • Zheng Li,
  • Qingnuan Li

摘要

The CLDN18.2 protein, which is highly expressed in tumors such as gastric cancer, has emerged as a critical molecular target for the development of anti-cancer diagnostic and therapeutic drugs. The CLDN18.2-targeted peptide radiopharmaceutical [131I]I-yg-15 was prepared and evaluated in this study. Molecular docking simulations reveal the binding site between the peptide and the CLDN18.2 protein at the atomic level. Under optimized preparation conditions, [131I]I-yg-15 achieved a labeling efficiency of 96.86 ± 1.34% and a specific activity of 5.63 GBq/μmol. In CLDN18.2-overexpressing cells, cellular uptake within 1 h was 3.31 ± 0.14%, significantly higher than that in the blocking group (1.0 ± 0.39%). SPECT-CT imaging and biodistribution studies confirmed that [131I]I-yg-15 specifically targeted and accumulated in CLDN18.2-positive tumor tissues, with a 1-h SUV of 0.41 ± 0.04, initially demonstrating the feasibility of peptide radiopharmaceuticals for the diagnosis and treatment of 18.2-positive tumors.