Mammalian bombesin (Bn) receptors comprise 3 subtypes: BB₁, BB₂, BB₃ (nomenclature recommended by the NC-IUPHAR Subcommittee on bombesin receptors, [11]). BB₁ and BB₂ are activated by the endogenous ligands neuromedin B (NMB, P08949) (NMB), gastrin-releasing peptide (GRP, P07492) (GRP), and GRP-(18-27) (GRP, P07492). Bombesin is a tetra-decapeptide, originally derived from amphibians. The three Bn receptor subtypes couple primarily to the G_q/11 and G_12/13 family of G proteins [11]. Each of these receptors is widely distributed in the CNS and peripheral tissues [7,11,31,34,38,46]. Activation of BB₁ and BB₂ receptors causes a wide range of physiological/pathophysiogical actions, including the stimulation of normal and neoplastic tissue growth, smooth-muscle contraction, gastrointestinal motility, feeding behavior, secretion and many central nervous system effects including regulation of circadian rhythm, body temperature control, sighing and mediation of pruritus [3,5,11,15,25,28,32,34,40,44]. A physiological role for the BB₃ receptor has yet to be fully defined although recently studies suggest an important role in glucose and insulin regulation, metabolic homeostasis, feeding, regulation of body temperature, obesity, diabetes mellitus and growth of normal/neoplastic tissues [7,14,18,26,30,45]. Bn receptors are one of the most frequently overexpressed receptors in cancers and are receiving increased attention for their roles in tumor growth, as well as for tumour imaging and for receptor targeted cytotoxicity [1,17,28,37].

All three human subtypes may be activated by [D-Phe⁶,β-Ala¹¹,Phe¹³,Nle¹⁴]bombesin-(6-14) [21]. Agonists [D-Tyr⁶,Apa-4Cl11,Phe¹³,Nle1⁴]bombesin-(6-14) has more than 200-fold selectivity for BB₃ receptors over BB₁ and BB₂ [20-21,34,34-35].

* Key recommended reading is highlighted with an asterisk

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* González N, Moreno P, Jensen RT. (2015) Bombesin receptor subtype 3 as a potential target for obesity and diabetes. Expert Opin Ther Targets, 19 (9): 1153-70. [PMID:26066663]

Guo M, Qu X, Qin XQ. (2015) Bombesin-like peptides and their receptors: recent findings in pharmacology and physiology. Curr Opin Endocrinol Diabetes Obes, 22 (1): 3-8. [PMID:25517020]

* Jensen RT, Battey JF, Spindel ER, Benya RV. (2008) International Union of Pharmacology. LXVIII. Mammalian bombesin receptors: nomenclature, distribution, pharmacology, signaling, and functions in normal and disease states. Pharmacol Rev, 60 (1): 1-42. [PMID:18055507]

Jensen RT, Moody TW. (2013) Bombesin Peptides (Cancer). In Handbook of Biologically Active Peptides. 2nd Revised edition. Edited by Kastin AJ (Elsevier) 506-511. [ISBN:9780123850959]

Jensen RT, Moody TW. (2013) Bombesin-Related Peptides. In Handbook of Biologically Active Peptides. 2nd Revised edition. Edited by Kastin AJ (Elsevier) 1188-1196. [ISBN:9780123850959]

Ladenheim EE. (2013) Bombesin. In Handbook of Biologically Active Peptides. 2nd Revised edition. Edited by Kastin AJ (Elsevier) 1064-1070. [ISBN:9780123850959]

* Li M, Liang P, Liu D, Yuan F, Chen GC, Zhang L, Liu Y, Liu H. (2019) Bombesin Receptor Subtype-3 in Human Diseases. Arch Med Res, 50 (7): 463-467. [PMID:31911345]

* Maina T, Nock BA, Kulkarni H, Singh A, Baum RP. (2017) Theranostic Prospects of Gastrin-Releasing Peptide Receptor-Radioantagonists in Oncology. PET Clin, 12 (3): 297-309. [PMID:28576168]

* Moreno P, Ramos-Álvarez I, Moody TW, Jensen RT. (2016) Bombesin related peptides/receptors and their promising therapeutic roles in cancer imaging, targeting and treatment. Expert Opin Ther Targets, 20 (9): 1055-73. [PMID:26981612]

* Qu X, Wang H, Liu R. (2018) Recent insights into biological functions of mammalian bombesin-like peptides and their receptors. Curr Opin Endocrinol Diabetes Obes, 25 (1): 36-41. [PMID:29120926]

* Ramos-Álvarez I, Moreno P, Mantey SA, Nakamura T, Nuche-Berenguer B, Moody TW, Coy DH, Jensen RT. (2015) Insights into bombesin receptors and ligands: Highlighting recent advances. Peptides, 72: 128-44. [PMID:25976083]

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Subcommittee members: Robert T. Jensen (Chairperson) National Institute of Diabetes & Kidney Diseases National Institutes of Health Building 10 Room 9C-103 NIH Bethesda MD 20892 USA Jim Battey National Institute on Deafness and Other Communication Disorders Building 31 Room 3C02 NIH Bethesda MD 20892 USA Richard V. Benya University of Illinois Section of Digestive Diseases and Nutrition 840 South Wood Street (M/C 716) Chicago Illinois 60612 USA Terry W. Moody National Institutes of Health Center for Cancer Research Bethesda MD USA