grpr

PSMA/GRPR ligand 1 (compound 3) is a bispecific ligand with dual targeting capabilities for tumors that express PSMA(+) and GRPR(+).

GRPR antagonist-1 is a potent antagonist of the gastrin-releasing peptide receptor (GRPR) and displays cytotoxicity to certain cancer cells, including PC3 cells (IC50: 4.97 μM), Pan02 cells (IC50: 4.36 μM), and HGC-27 cells (IC50: 3.40 μM). It reduces Bcl-2 levels, increases Bax levels, inhibits HGC-27 cell viability, and induces apoptosis, thereby exhibiting anti-cancer effects.

GRPR antagonist-2 is a potent antagonist of the gastrin-releasing peptide receptor (GRPR) and exhibits anticancer effects with cytotoxicity to HGC-27 cells (IC50: 0.77 μM) and Pan02 cells (IC50: 2.5 μM).

GB-6, a short linear peptide that selectively binds to the gastrin releasing peptide receptor (GRPR), shows potential as a high-contrast imaging probe due to its tumor selectivity and specific accumulation. Overexpression of GRPR in pancreatic cancer enables GB-6, when labeled with near-infrared (NIR) fluorescent dyes or the radionuclide technetium-99m (99mTc), to serve as an effective agent for tumor visualization. Demonstrating excellent in vivo stability, GB-6 yields tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW1990 subcutaneous xenograft models. Its rapid tumor targeting capability and precise tumor boundary delineation signify GB-6's extensive potential for clinical applications [1].

PD176252 is a potent BB1 and BB2 antagonist with inhibitory effects on BB1 and BB2 receptors.PD176252 acts as a small molecule GRPR inhibitor and FPR1/FPR2 agonist to inhibit the growth and proliferation of a variety of cancer cells.

NOTA-P2-RM26 is a high-affinity NOTA-conjugated bombesin antagonist designed for GRPR-targeted tumor imaging.

AMTG-DA1 is a ligand for the gastrin-releasing peptide receptor (GRPR), and it can be utilized in cancer research.

BA 1 TFA acts as a potent agonist for the bombesin (BB) family of receptors, exhibiting high affinity binding to Bombesin receptor subtype-3 (BRS3), gastrin-releasing peptide receptor (GRPR), and neuromedin B receptor (NMBR), with IC50 values of 6, 0.4, and 2.5 nM, respectively [1].

[Lys3]-Bombesin is a biologically active peptide used in PET (Positron Emission Tomography) imaging to identify GRPR (gastrin-releasing peptide receptor) positive prostate cancer. The compound, when conjugated with a corresponding monoclonal antibody, can selectively trigger CD64-dependent monocyte and neutrophil-mediated lysis in small cell carcinoma.

PD 168368 is a novel, potent, competitive and selective nonpeptide neuromodulin B receptor (NMB-R) antagonist with inhibitory effects on the gastrin-releasing peptide receptor (GRPR).PD 168368 is a potent mixed agonist of FPR1/FPR2/FPR3.

RC-3095, a selective GRPR antagonist, has been shown to have anti-inflammatory properties in different models of inflammation.

Mammalian bombesin-like peptide neurotransmitter that is an agonist for the gastrin-releasing peptide receptor (GRPR). GRP has been reported to activate GABAergic interneurons in the amygdala leading to increased GABA release and fear suppression in mice

RC-3095 acetate is an antagonist of bombesin gastrin-releasing peptide receptor (GRPR). It exerts protective effects by reducing gastric oxidative injury in the arthritic mice.