Substitution of L-Trp by α-methyl-L-Trp in 177Lu-RM2 results in 177Lu-AMTG, a high affinity GRPR ligand with improved in vivo stability

T Guenther, S Deiser, V Felber, R Beck… - Journal of Nuclear …, 2022 - Soc Nuclear Med
Theranostic applications targeting the gastrin-releasing peptide receptor (GRPR) have
shown promising results. When compared with other peptide ligands for radioligand therapy …

Substitution of L-tryptophan by α-methyl-L-tryptophan in 177Lu-RM2 results in 177Lu-AMTG, a high-affinity gastrin-releasing peptide receptor ligand with improved in …

T Günther, S Deiser, V Felber, R Beck… - Journal of Nuclear …, 2022 - Soc Nuclear Med
Theranostic applications targeting the gastrin-releasing peptide receptor (GRPR) have
shown promising results. When compared with other peptide ligands for radioligand therapy …

Preclinical comparison of the 64Cu-and 68Ga-labeled GRPR-targeted compounds RM2 and AMTG, as well as first-in-humans [68Ga] Ga-AMTG PET/CT

L Koller, M Joksch, S Schwarzenböck… - Journal of Nuclear …, 2023 - Soc Nuclear Med
Despite the recent success of prostate-specific membrane antigen (PSMA)–targeted
compounds for theranostic use in prostate cancer (PCa), alternative options for the detection …

68Ga/177Lu-NeoBOMB1, a novel radiolabeled GRPR antagonist for theranostic use in oncology

SU Dalm, IL Bakker, E de Blois… - Journal of Nuclear …, 2017 - Soc Nuclear Med
Because overexpression of the gastrin-releasing peptide receptor (GRPR) has been
reported on various cancer types, for example, prostate cancer and breast cancer, targeting …

[HTML][HTML] Preclinical evaluation of new GRPR-antagonists with improved metabolic stability for radiotheranostic use in oncology

P Kanellopoulos, A Mattsson, A Abouzayed… - EJNMMI …, 2024 - Springer
Background The gastrin-releasing peptide receptor (GRPR) has been extensively studied as
a biomolecular target for peptide-based radiotheranostics. However, the lack of metabolic …

99mTc radiotracers based on human GRP (18-27): synthesis and comparative evaluation

PJ Marsouvanidis, T Maina, W Sallegger… - Journal of Nuclear …, 2013 - Soc Nuclear Med
Gastrin-releasing peptide receptors (GRPRs) expressed on human tumors can serve as
molecular targets for radiolabeled peptide analogs based on the frog tetradecapeptide …

[HTML][HTML] Side-by-side comparison of the two widely studied GRPR radiotracers, radiolabeled NeoB and RM2, in a preclinical setting

TST Damiana, P Paraïso, C de Ridder… - European Journal of …, 2023 - Springer
Introduction NeoB and RM2 are the most investigated gastrin-releasing peptide receptor
(GRPR)–targeting radiotracers in preclinical and clinical studies. Therefore, an extensive …

Preclinical Evaluation of Gastrin-Releasing Peptide Receptor Antagonists Labeled with 161Tb and 177Lu: A Comparative Study

N Holzleitner, T Cwojdzinski, R Beck… - Journal of Nuclear …, 2024 - Soc Nuclear Med
To elucidate potential benefits of the Auger-electron–emitting radionuclide 161Tb, we
compared the preclinical performance of the gastrin-releasing peptide receptor antagonists …

Approaches to improve metabolic stability of a statine-based GRP receptor antagonist

I Popp, L Del Pozzo, B Waser, JC Reubi… - Nuclear medicine and …, 2017 - Elsevier
The bombesin receptor family, in particular the gastrin-releasing peptide receptor (GRPr), is
an attractive target in the field of nuclear oncology due to the high density of these receptors …

[HTML][HTML] Unnatural amino acid substitutions to improve in vivo stability and tumor uptake of 68Ga-labeled GRPR-targeted TacBOMB2 derivatives for cancer imaging …

L Wang, HT Kuo, Z Zhang, C Zhang, CC Chen… - EJNMMI …, 2024 - Springer
Background Overexpressed in various solid tumors, gastrin-releasing peptide receptor
(GRPR) is a promising cancer imaging marker and therapeutic target. Although antagonists …