1. Signaling Pathways
  2. GPCR/G Protein
  3. Bombesin Receptor

Bombesin Receptor

Bombesin, a peptide of 14 amino acids, is an amphibian homolog to the mammalian gastrin-releasing peptide (GRP), that has been extensively studied as a targeting ligand for diagnosis and therapy of GRP positive tumors, such as breast, pancreas, lungs and prostate cancers. Bombesin binds to and activates G-protein coupled receptors, known as gastrin releasing peptide receptor (GRPR).

Bombesin, a tetradecapeptide isolated from the skin of the frog Bombina bombina, have shown broad spectrum of biological activities. The BBS activates three G protein-coupled receptors: bombesin receptor 1 (BB1), bombesin receptor 2 (BB2), and bombesin receptor 3 (BB3). BBS-like peptides-Neuromedin B (NB) and gastrin releasing peptide (GRP) are natural ligand of the BB1 and BB2 receptors, respectively.

In mammals, BBS receptors and BBS-like peptides are distributed in the Central Nervous System (CNS) including regions involved in the cardiorespiratory control.

The mammalian bombesin G-protein-coupled receptor subfamily comprises three structurally related members, the receptors for neuromedin B (NMBR or BB1), gastrin-releasing peptide (GRPR or BB2), and bombesin receptor subtype-3 (BRS-3 or BB3).

Bombesin receptor subtype-3 (BRS-3) is an orphan G protein-coupled receptor implicated in the regulation of energy homeostasis.

Bombesin Receptor Related Products (8):

Cat. No. Product Name Effect Purity
  • HY-14342
    MK-5046 Agonist 99.67%
    MK-5046 is a novel BRS-3 agonist, binds to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM).
  • HY-P0195
    Bombesin Modulator 99.69%
    Bombesin is a tetradecapeptide originally isolated from frog skin; plays an important role in the release of gastrin and the activation of G-protein receptors.
  • HY-103286
    PD176252 Antagonist >99.0%
    PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
  • HY-P0107
    RC-3095 Antagonist
    RC-3095 is a bombesin/gastrin releasing peptide receptor antagonist.
  • HY-N4247
    Kuwanon G Antagonist
    Kuwanon G is a flavonoid isolated from Morus alba, acts as a bombesin receptor antagonist, with potential antimicrobial activity.
  • HY-N2600
    Kuwanon H Antagonist
    Kuwanon H is a flavonoid isolated from Morus bombycis, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells.
  • HY-101844
    ML-18 Antagonist 98.04%
    ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
  • HY-P0107A
    RC-3095 (TFA) Antagonist
    RC-3095 TFA is a bombesin/gastrin releasing peptide receptor antagonist.
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