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The effects of novel macrocyclic chelates on the targeting properties of the 68Ga-labeled Gastrin releasing peptide receptor antagonist RM2.

Yinwen Wang | Hongmei Yuan | Sufan Tang | Yang Liu | Ping Cai | Nan Liu | Yue Chen | Zhijun Zhou
EJNMMI research | 2023

The gastrin-releasing peptide receptor (GRPr) is a molecular target for the visualization of prostate cancer. Bombesin (BN) analogs are short peptides with a high affinity for GRPr. RM2 is a bombesin-based antagonist. It has been demonstrated that RM2 have superior in vivo biodistribution and targeting properties than high-affinity receptor agonists. This study developed new RM2-like antagonists by introducing the novel bifunctional chelators AAZTA5 and DATA5m to RM2.

Pubmed ID: 37285007

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Associated grants

  • Agency: the National Natural Science Foundation of China,
    Id: U20A20384
  • Agency: Sichuan Province Science and Technology Support Program,
    Id: 2021YJ0131

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