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

ABSTRACT:

Background

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 DATA^5m to RM2.

Results

The effects of different macrocyclic chelating groups on drug targeting properties and the possibility of preparing ⁶⁸Ga-radiopharmaceuticals in a kit-based protocol were investigated using ⁶⁸Ga-labeled entities. Both new RM2 variants were labelled

SUBMITTER: Wang Y 

PROVIDER: S-EPMC10247930 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature