Of the 22 prostate cancer specimens analyzed by RT-PCR, 20 (91%) expressed GRPR mRNA, 3 (14%) showed NMBR mRNA, and 2 ( approximately 9%) revealed BRS-3 mRNA.
We have further investigated the effect of androgen modulation on GRPR-expression in three androgen-dependent human PC-bearing xenografts: PC295, PC310 and PC82 using the androgen-independent PC3-model as a reference.
We sought to evaluate the tumor binding and imaging potential of (177)Lu-AMBA in low GRP-R models of prostate cancer and determine how reduced expression affects (177)Lu-AMBA radiotherapy efficacy.
These findings constitute a caveat for the use of GRPR as a target for diagnostic or therapeutic approaches to high grade or progressed prostate cancer.
Immunohistochemical analysis of gastrin-releasing peptide receptor (GRPR) and possible regulation by estrogen receptor βcx in human prostate carcinoma.
This study indicates the safety and efficiency of a new type of dual integrin α<sub>v</sub>β<sub>3</sub>- and GRPR-targeting PET radiotracer in prostate cancer diagnosis and staging.
The GRPR antagonist radioligands <sup>67</sup>Ga-, <sup>111</sup>In-, and <sup>177</sup>Lu-NeoBOMB1, independent of the radiometal applied, have shown comparable behavior in prostate cancer models, in favor of future theranostic use in GRPR-positive cancer patients.
Considering their adequate imaging characteristics, [<sup>64</sup> Cu]-NOTA-LK-RM26 bearing APCA- and AHDA-linkers are promising candidates for GRPR-targeted PET imaging prostate cancer.
Despite still investigational, the bombesin-based radiotracers and antagonist of gastrin releasing-peptide receptor (GRP) (RM2) and anti1-amino-3-18Ffluorocyclobutane-1-carboxylic acid (18F-FACBC) are emerging as possible alternatives for investigating PCa.
Overall, the antagonistic GRPR targeted probe <sup>68</sup>Ga-NOTA-PEG<sub>3</sub>-RM26 is a more-promising candidate than the agonist <sup>68</sup>Ga-NOTA-Aca-BBN<sub>7-14</sub> for the PET imaging of prostate cancer patients.
We review the preclinical and clinical literatures on the use of GRPRs as targets for imaging and therapy of prostate cancer, with a focus on the newer developments and theranostic potential of GRPR peptides.
Gastrin-Releasing Peptide Receptor- and Prostate-Specific Membrane Antigen-Specific Ultrasmall Gold Nanoparticles for Characterization and Diagnosis of Prostate Carcinoma via Fluorescence Imaging.
<sup>68</sup>Ga-RM2 is a gastrin releasing peptide receptor (GRPR) antagonist PET (positron emission tomography) radiotracer which is being investigated in clinical trials as a potential prostate cancer imaging agent.
This study aimed to synthesize and characterize the Lu-DOTA-PSMA(inhibitor)-Lys-bombesin (Lu-DOTA-iPSMA-Lys-BN) heterodimer and to evaluate its potential to target prostate-specific membrane antigen (PSMA) and gastrin-releasing peptide receptor (GRPr) overexpressed in prostate cancer.
The gastrin-releasing peptide receptor (GRPR), a G protein-coupled receptor, is overexpressed in solid malignancies and particularly in prostate cancer.