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Bombesin and Analogs
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|B07020||(D-Tyr6,betaPhe11,Phe13,Nle14)-Bombesin (6-14) (free acid)||Inquiry|
Bombesin and analogs mainly include gastrin-releasing peptide (GRP), neuromedin C (NMC) and neuromedin B (NMB). Bombesin and its analogs are involved in the proliferation and differentiation of various tumors. Effective inhibition of bombesin is expected to be a new approach to tumor therapy. Bombesin was first discovered in the skin of frogs. The first mammalian bomberin-like peptide (BLP) is isolated from the gastrointestinal tract of the pig. It is named as GRP because of its role in promoting gastrin secretion. GRP contains 27 amino acids with 7 amino acids at the C-terminus identical to bombesin. NMC containing 10 amino acids was found to be identical to the 10 amino acids at the C-terminus of GRP. The BLP receptors found in normal mammals have two subtypes, the GRP-receptor (also known as BB2-receptor) and the NMB-receptor (also known as BB1-receptor). GRP-receptors have high affinity with GRP and NMC, but have low affinity with NMB. NMB-receptors have high affinity with NMB, but have low affinity with GRP and NMC.
Mechanism of action
The biological role of members of the BLP family is primarily mediated through GRP-R and NMB-R receptor subtypes. Since the active site of the BLP family of polypeptides is 10 amino acid residues at the C-terminus, differences in C-terminus may affect their biological function. BLP acts as a neurotransmitter in the pancreas to directly promote islet β-cells or indirectly through the activation of parasympathetic nerves to promote insulin secretion. BLP can also increase Ca2+ in the cytosol by increasing extracellular Ca2+ influx or mobilizing intracellular calcium stores. At the same time, the secretion of insulin is promoted through pathways such as phospholipase and protein kinase.
Application of Bombesin and Analogs
Since insulin plays a vital role in the metabolism of the body, the effects of BLP family members on insulin secretion have been deeply studied. Bombesin and analogs will provide new ideas for clinical treatment of diabetes.
1. Rozengurt, E. Bombesin-induction of cell proliferation in 3T3 Cells. (1988) Specific receptors and early signaling events. Ann N Y Acad Sci, 547: 277-292.