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<p>Gadolinium-neutron capture therapy (Gd-NCT) employs Gadolinium (Gd) isotopes and thermal neutrons to specifically target and kill cancer at cells level. This study investigates the targeting efficacy of <sup>157</sup>Gd-DOTA-HK (DHK), a novel agent designed for Gd-NCT and MRI. We synthesized <sup>157</sup>Gd-DHK, which combines a Gd-DOTA complex as a neutron capturer and MRI probe with αvβ6 binding peptide (HK) for targeted Pancreas adenocarcinoma (PDAC) therapy. <sup>157</sup>Gd-DHK demonstrated a significantly high binding affinity for BxPC-3 cells. scintigraphy revealed that the optimal time window for Gd-NCT was 26&#xa0;h after injection. The conjugate’s imaging capabilities and its potential as an MRI contrast agent were validated. The conjugate effectively triggered nuclear reactions via Gd-NCT, leading to efficient tumor cell destruction. Photon sensitization studies showed that <sup>157</sup>Gd-DHK induced photon-mediated phototoxicity in cancer cells while exhibiting minimal toxicity. <sup>157</sup>Gd-DHK shows great potential as a theranostic agent for targeted imaging of PDAC and Gd-NCT applications. It presents a novel strategy to enhance the specificity and efficacy of Gd-NCT in cancer treatment.</p>

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157Gd-DHK: enhancing targeted gadolinium neutron capture for pancreatic adenocarcinoma

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年12月4日

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  • Liang Xie,
  • Cuiping Song,
  • Jialin Qin,
  • Qianqian Xu,
  • Jianchun Yin,
  • Yuanyuan Ma,
  • Hong Chen,
  • Chao Li,
  • Bing Hong,
  • Ni Chen,
  • Xiaoxi Pang

摘要

Gadolinium-neutron capture therapy (Gd-NCT) employs Gadolinium (Gd) isotopes and thermal neutrons to specifically target and kill cancer at cells level. This study investigates the targeting efficacy of 157Gd-DOTA-HK (DHK), a novel agent designed for Gd-NCT and MRI. We synthesized 157Gd-DHK, which combines a Gd-DOTA complex as a neutron capturer and MRI probe with αvβ6 binding peptide (HK) for targeted Pancreas adenocarcinoma (PDAC) therapy. 157Gd-DHK demonstrated a significantly high binding affinity for BxPC-3 cells. scintigraphy revealed that the optimal time window for Gd-NCT was 26 h after injection. The conjugate’s imaging capabilities and its potential as an MRI contrast agent were validated. The conjugate effectively triggered nuclear reactions via Gd-NCT, leading to efficient tumor cell destruction. Photon sensitization studies showed that 157Gd-DHK induced photon-mediated phototoxicity in cancer cells while exhibiting minimal toxicity. 157Gd-DHK shows great potential as a theranostic agent for targeted imaging of PDAC and Gd-NCT applications. It presents a novel strategy to enhance the specificity and efficacy of Gd-NCT in cancer treatment.