Bombesin Receptor Subtype-3 in Human Diseases

This review summarizes the recent findings of the roles of bombesin receptor subtype-3 (BRS-3) in various patho-physiological conditions. Studies have demonstrated that two mammalians bombesin-like peptides, GRP and NMB, exhibit a large range of functions by binding to three receptors. Knockout studies showed that the mice BRS-3 has important effects on tumor growth, energy homeostasis, glucose regulation, satiety, and lung development (1,7). BRS-3 is an orphan receptor whose natural ligand is unknown. However, several agonists and antagonists have been synthesized which facilitate its characterization, (D-Tyr6, β-Ala11, Phe13, Nle14) Bn-(6-14) and MK-5046 are agonists, whereas ML-18 and Bantag-1 are antagonists. With the development of several selective, high-affinity BRS-3 agonists and antagonists, recent studies provided some insights into the biological effects of BRS-3 in several disease states including lung cancer, obesity, diabetes mellitus, asthma, and kidney diseases.