More information on this family may be found on the IUPHAR-DB family and introduction pages.
Bombesin receptors (nomenclature recommended by the NC-IUPHAR Subcommittee on bombesin receptors, [4]) are activated by the endogenous ligands gastrin-releasing peptide (GRP), NMB (NMB) and GRP-(18-27) (previously named neuromedin C). bombesin is a tetradecapeptide, originally derived from amphibians. These receptors couple primarily to the Gq/11 family of G proteins (but see also [5]). Activation of BB1 and BB2 receptors causes a wide range of physiological actions, including the stimulation of tissue growth, smooth–muscle contraction, secretion and many central nervous system effects [12]. A physiological role for the BB3 receptor has yet to be fully defined although receptor knockout experiments suggest a role in energy balance and the control of body weight [4].
Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Receptors 
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Iwabuchi, M., Ui-Tei, K., Yamada, K., Matsuda, Y., Sakai, Y., Tanaka, K. and Ohki-Hamazaki, H. (2003) Molecular cloning and characterization of avian bombesin-like peptide receptors: New tools for investigating molecular basis for ligand selectivity. Br J Pharmacol., 139: 555-566. [PMID:12788815]
Jensen, R. T. and Coy, D. H. (1991) Progress in the development of potent bombesin receptor antagonists. Trends Pharmacol Sci, 12: 13-19. [PMID:1706545]
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]
Kroog, GS; Jensen, RT; Battey, JF. (1995) Mammalian bombesin receptors. Med Res Rev, 15 (5): 389-417. [PMID:8531502]
Moody, T. W. and Merali, Z. (2004) Bombesin-like peptides and associated receptors within the brain: distribution and behavioral implications. Peptides, 25: 511-520. [PMID:15134870]
Moody, T. W., Mantey, S. A., Pradhan, T. K., Schumann, M., Nakagawa, T., Martinez, A., Fuselier, J., Coy, D. H. and Jensen, R. T. (2004) Development of high affinity camptothecin-bombesin conjugates that have targeted cytotoxicity for bombesin receptor-containing tumor cells. J Biol Chem, 279: 23580-23589. [PMID:15016826]
Ohki-Hamazaki, H. (2000) Neuromedin B. Prog Neurobiol, 62: 297-312. [PMID:10840151]
Ohki-Hamazaki, H; Iwabuchi, M; Maekawa, F. (2005) Development and function of bombesin-like peptides and their receptors. Int. J. Dev. Biol., 49 (2-3): 293-300. [PMID:15906244]
Roesler, R., Henriques, J. A. and Schwartsmann, G. (2006) Gastrin-releasing peptide receptor as a molecular target for psychiatric and neurological disorders. CNS Neurol Disord Drug Targets, 5: 197-204. [PMID:16611092]
Tokita, K., Hocart, S. J., Coy, D. H. and Jensen, R. T. (2002) Molecular basis of the selectivity of gastrin-releasing peptide receptor for gastrin-releasing peptide. Mol Pharmacol, 61: 1435-1443. [PMID:12021405]
Wada, E., Way, J., Shapira, H. and Battey, J. F. (1992) Two distinct bombesin receptor subtypes in postnatal rat central nervous system. Mol. Cell. Neurosci., 3: 446-460. [PMID:1726343]
Weber, D., Berger, C., Eickelmann, P., Antel, J. and Kessler, H. (2003) Design of selective peptidomimetic agonists for the human orphan receptor BRS-3. J Med Chem., 46: 1918-1930. [PMID:12723954]
Weber, HC. (2009) Regulation and signaling of human bombesin receptors and their biological effects. Curr Opin Endocrinol Diabetes Obes, 16 (1): 66-71. [PMID:19115523]
Zhou, J; Chen, J; Mokotoff, M; Ball, ED. (2004) Targeting gastrin-releasing peptide receptors for cancer treatment. Anticancer Drugs, 15 (10): 921-7. [PMID:15514561]
1. Benya, R. V., Kusui, T., Pradhan, T. K., Battey, J. F. and Jensen, R. T. (1995) Expression and characterization of cloned human bombesin receptors. Mol Pharmacol., 47: 10-20. [PMID:7838118]
2. Eden, J. M. et al.. (1996) PD 165929. The first high affinity non-peptide neuromedin_B receptor antagonist. Bioorganic and Medicinal Chemistry Letters., 6: 2617-2622.
3. Heimbrook, D. C., Saari, W. S., Balishin, N. L., Friedman, A., Moore, K. S., Reimen, M. W., Kiefer, D. M., Rotberg, N. S., Wallen, J. W. and Oliff, A. (1989) Carboxyl-terminal modification of a gastrin releasing peptide derivativegenerates potent antagonists. J Biol Chem., 264: 11258-11262. [PMID:2544588]
4. 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]
5. Jian, X; Sainz, E; Clark, WA; Jensen, RT; Battey, JF; Northup, JK. (1999) The bombesin receptor subtypes have distinct G protein specificities. J. Biol. Chem., 274 (17): 11573-81. [PMID:10206964]
6. Llinares, M., Devin, C., Chaloin, O., Azay, J., Noel-Artis, A. M., Bernad, N., Fehrentz, J. A. and Martinez, J. (1999) Syntheses and biological activities of potent bombesin receptor antagonists. J Pept Res., 53: 275-283. [PMID:10231715]
7. Mantey, S. A., Coy, D. H., Entsuah, L. K. and Jensen, R. T. (2004) Development of Bombesin Analogues With Conformationally-Restricted Amino Acid Substitutions With Enhanced Selectivity for the Orphan Receptor, hBRS-3. J Pharmacol Exp Ther., 310: 1161-1170. [PMID:15102928]
8. Mantey, S. A., Weber, H. C., Sainz, E., Akeson, M., Ryan, R. R., Pradhan, T. K., Searles, R. P., Spindel, E. R., Battey, J. F., Coy, D. H. and Jensen, R. T. (1997) Discovery of a high affinity radioligand for the human orphan receptor, bombesin receptor subtype 3, which demonstrates that it has a uniquepharmacology compared with other mammalian bombesin receptors. J Biol Chem., 272: 26062-26071. [PMID:9325344]
9. Mantey, S., Frucht, H., Coy, D. H. and Jensen, R. T. (1993) Characterization of bombesin receptors using a novel, potent, radiolabeled antagonist that distinguishes bombesin receptor subtypes. Mol Pharmacol., 43: 762-774. [PMID:7684815]
10. Orbuch, M., Taylor, J. E., Coy, D. H., Mrozinski, J. E. Jr., Mantey, S. A., Battey, J. F., Moreau, J. P. and Jensen, R. T. (1993) Discovery of a novel class of neuromedin B receptor antagonists, substituted somatostatin analogues. Mol Pharmacol., 44: 841-850. [PMID:7901752]
11. Ryan, R., Katsuno, T., Mantey, S. A., Pradhan, T. K., Weber, H. C., Coy, D. H., Battey, J. F. and Jensen, R. T. (1999) Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD168368. J Pharmacol Exp Ther., 290: 1202-1211. [PMID:10454496]
12. Tokita, K., Hocart, S. J., Coy, D. H. and Jensen, R. T. (2002) Molecular basis of the selectivity of gastrin-releasing peptide receptor for gastrin-releasing peptide. Mol Pharmacol, 61: 1435-1443. [PMID:12021405]
13. Tokita, K., Katsuno, T., Hocart, S. J., Coy, D. H., Llinares, M., Martinez, J. and Jensen, R. T. (2001) Molecular basis for selectivity of high affinity peptide antagonists for the gastrin-releasing peptide receptor. J Biol Chem., 276: 36652-36663. [PMID:11463790]
14. Wada, E., Way, J., Shapira, H., Kusano, K., Lebacq-Verheyden, A. M., Coy, D., Jensen, R. and Battey, J. F. (1991) cDNA cloning, characterization, and brain region-specific expression of a neuromedin-B-preferring bombesin receptor. Neuron, 6: 421-430. [PMID:1848080]
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All three subtypes may be activated by [D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) [8]. [D-Tyr6,Apa-4Cl11,Phe13,Nle14]bombesin-(6-14) has more than 200-fold selectivity for BB3 receptors over BB1 and BB2 [7].