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BB3 receptor

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Target id: 40

Nomenclature: BB3 receptor

Family: Bombesin receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 399 Xq26.3 BRS3 bombesin receptor subtype 3 5,11
Mouse 7 399 X A6 Brs3 bombesin-like receptor 3 32,46
Rat 7 399 Xq37 Brs3 bombesin receptor subtype 3 18
Previous and Unofficial Names Click here for help
bb3 | bombesin receptor subtype-3 | bombesin like receptor 3
Database Links Click here for help
Specialist databases
GPCRdb brs3_human (Hs), brs3_mouse (Mm), brs3_rat (Rn)
Other databases
Alphafold P32247 (Hs), O54798 (Mm), Q8K418 (Rn)
ChEMBL Target CHEMBL4080 (Hs), CHEMBL1075140 (Mm), CHEMBL1075111 (Rn)
Ensembl Gene ENSG00000102239 (Hs), ENSMUSG00000031130 (Mm), ENSRNOG00000000873 (Rn)
Entrez Gene 680 (Hs), 12209 (Mm), 260319 (Rn)
Human Protein Atlas ENSG00000102239 (Hs)
KEGG Gene hsa:680 (Hs), mmu:12209 (Mm), rno:260319 (Rn)
OMIM 300107 (Hs)
Pharos P32247 (Hs)
RefSeq Nucleotide NM_001727 (Hs), NM_009766 (Mm), NM_152845 (Rn)
RefSeq Protein NP_001718 (Hs), NP_033896 (Mm), NP_690058 (Rn)
UniProtKB P32247 (Hs), O54798 (Mm), Q8K418 (Rn)
Wikipedia BRS3 (Hs)

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]bag-2 Small molecule or natural product Primary target of this compound Ligand is labelled Ligand is radioactive Mm Agonist 8.6 pKd 12
⤷ pKd 8.6 (Kd 2.6x10-9 M) [12]
[125I][D-Tyr6,β-Ala11,Phe13,Nle14]bombesin-(6-14) Peptide Ligand is labelled Ligand is radioactive Hs Full agonist 8.0 – 8.4 pKd 23,29
⤷ pKd 8.0 – 8.4 (Kd 1x10-8 – 3.98x10-9 M) [23,29]
[D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) Peptide Rn Full agonist 9.0 pKi 39
⤷ pKi 9.0 (Ki 1x10-9 M) [39]
[D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) Peptide Mm Full agonist 8.8 pKi 39
⤷ pKi 8.8 (Ki 1.5x10-9 M) [39]
MK-5046 Small molecule or natural product Mm Full agonist 8.8 pKi 13
⤷ pKi 8.8 (Ki 1.6x10-9 M) [13]
[D-Tyr6,(R)-APA11,Phe13,Nle14]bombesin-(6-14) Peptide Hs Full agonist 8.4 pKi 22
⤷ pKi 8.4 (Ki 4.1x10-9 M) [22]
[D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) Peptide Click here for species-specific activity table Hs Full agonist 8.1 – 8.4 pKi 23
⤷ pKi 8.1 – 8.4 (Ki 8.9x10-9 – 4.2x10-9 M) [23]
[D-Tyr6,Apa-4Cl11,Phe13,Nle14]bombesin-(6-14) Peptide Hs Full agonist 8.1 pKi 21
⤷ pKi 8.1 (Ki 8x10-9 M) [21]
MK-5046 Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.7 – 8.4 pKi 29,43
⤷ pKi 7.7 – 8.4 [29,43]
compound 21b [PMID: 12723954] Small molecule or natural product Hs Full agonist 9.2 – 10.2 pEC50 46
⤷ pEC50 9.2 – 10.2 [46]
compound 9g [PMID: 24412111] Small molecule or natural product Hs Agonist 8.8 pEC50 25,35,38
⤷ pEC50 8.8 (EC50 1.7x10-9 M) [25,35,38]
phenylacetyl-Ala,DTrp-phenthylamide Small molecule or natural product Hs Full agonist 7.8 – 8.9 pEC50 47,50
⤷ pEC50 7.8 – 8.9 (EC50 1.415x10-8 – 1.2x10-9 M) [47,50]
compound 17c [PMID: 25497965] Small molecule or natural product Primary target of this compound Hs Agonist 7.9 pEC50 24
⤷ pEC50 7.9 (EC50 1.2x10-8 M) [24]
compound 9f [PMID: 24412111] Small molecule or natural product Primary target of this compound Hs Agonist 7.8 pEC50 25
⤷ pEC50 7.8 (EC50 1.7x10-8 M) [25]
MK-5046 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.6 pEC50 43
⤷ pEC50 7.6 (EC50 2.5x10-8 M) [43]
phenylacetyl-Ala,DTrp-phenthylamide Small molecule or natural product Mm Full agonist 7.5 pEC50 50
⤷ pEC50 7.5 (EC50 3.33x10-8 M) [50]
Ac-Phe-Trp-Ala-His(τBZL)-Nip-Gly-Arg-NH2 Peptide Hs Full agonist 6.4 – 8.2 pEC50 2,9,42
⤷ pEC50 6.4 – 8.2 (EC50 3.98x10-7 – 6.9x10-9 M) [2,9,42]
compound A [PMID: 28324017] Small molecule or natural product Rn Agonist 7.0 pEC50 31
⤷ pEC50 7.0 (EC50 1x10-7 M) [31]
Description: In a Ca aequorin assay.
phenylacetyl-Ala,DTrp-phenthylamide Small molecule or natural product Rn Full agonist 7.0 pEC50 50
⤷ pEC50 7.0 (EC50 1.099x10-7 M) [50]
compound A [PMID: 28324017] Small molecule or natural product Hs Agonist 6.6 pEC50 31
⤷ pEC50 6.6 (EC50 2.5x10-7 M) [31]
Description: In a Ca aequorin assay.
NMU (104-114) Peptide Hs Agonist 5.7 pEC50 7
⤷ pEC50 5.7 (EC50 2.19x10-6 M) [7]
compound 8a [PMID: 24900283] Small molecule or natural product Primary target of this compound Hs Agonist 8.9 pIC50 19
⤷ pIC50 8.9 (IC50 1.4x10-9 M) [19]
bag-1 Small molecule or natural product Rn Full agonist 8.6 pIC50 12
⤷ pIC50 8.6 (IC50 2.4x10-9 M) [12]
MK-7725 Small molecule or natural product Primary target of this compound Hs Agonist 8.5 pIC50 4
⤷ pIC50 8.5 (IC50 3x10-9 M) [4]
bag-2 Small molecule or natural product Mm Full agonist 8.2 pIC50 12
⤷ pIC50 8.2 (IC50 6.6x10-9 M) [12]
bag-1 Small molecule or natural product Mm Full agonist 8.2 pIC50 12
⤷ pIC50 8.2 (IC50 6.9x10-9 M) [12]
[D-Tyr6,Apa-4Cl11,Phe13,Nle14]bombesin-(6-14) Peptide Hs Full agonist 7.4 – 8.9 pIC50 9,42
⤷ pIC50 7.4 – 8.9 (IC50 4x10-8 – 1.4x10-9 M) [9,42]
bag-2 Small molecule or natural product Rn Full agonist 8.0 pIC50 12
⤷ pIC50 8.0 (IC50 1.03x10-8 M) [12]
[D-Tyr6,(R)-APA11,Phe13,Nle14]bombesin-(6-14) Peptide Hs Full agonist 7.5 – 8.4 pIC50 9,42
⤷ pIC50 7.5 – 8.4 (IC50 2.95x10-8 – 4.3x10-9 M) [9,42]
bag-1 Small molecule or natural product Hs Agonist 7.7 pIC50 12
⤷ pIC50 7.7 (IC50 1.83x10-8 M) [12]
compound 22e [PMID: 20167483] Small molecule or natural product Primary target of this compound Hs Agonist 7.6 pIC50 14
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [14]
MK-5046 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.8 – 7.6 pIC50 29,43
⤷ pIC50 6.8 – 7.6 (IC50 1.6x10-7 – 2.7x10-8 M) [29,43]
bag-2 Small molecule or natural product Hs Agonist 7.0 pIC50 12
⤷ pIC50 7.0 (IC50 9.6x10-8 M) [12]
Ac-Phe-Trp-Ala-His(τBZL)-Nip-Gly-Arg-NH2 Peptide Hs Full agonist 6.2 – 7.3 pIC50 9,42
⤷ pIC50 6.2 – 7.3 (IC50 5.72x10-7 – 4.9x10-8 M) [9,42]
phenylacetyl-Ala,DTrp-phenthylamide Small molecule or natural product Hs Full agonist 5.0 – 5.5 pIC50 42
⤷ pIC50 5.0 – 5.5 (IC50 1x10-5 – 3.162x10-6 M) [42]
View species-specific agonist tables
Agonist Comments
[D-Phe6,β-Ala11,Phe13,Nle14]bombesin(6-14) has a low affinity for rat and mouse BB3 receptors (pKd 5.70) whereas it has high affinity for the chicken BB3 (pKd 9.13) similar to its affinity for the human receptor [15,18].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]bantag-1 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.6 pKi 36
⤷ pKi 9.6 [36]
bantag-1 Small molecule or natural product Rn Antagonist 8.8 pIC50 12
⤷ pIC50 8.8 (IC50 1.7x10-9 M) [12]
bantag-1 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 – 8.7 pIC50 12,29,36
⤷ pIC50 8.6 – 8.7 (IC50 2.5x10-9 – 2x10-9 M) [12,29,36]
bantag-1 Small molecule or natural product Mm Antagonist 8.1 pIC50 12
⤷ pIC50 8.1 (IC50 8.1x10-9 M) [12]
D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2 Peptide Click here for species-specific activity table Hs Antagonist 5.6 pIC50 23,40-41
⤷ pIC50 5.6 [23,40-41]
ML-18 Small molecule or natural product Hs Antagonist 5.3 pIC50 27
⤷ pIC50 5.3 (IC50 4.8x10-6 M) [27]
View species-specific antagonist tables
Antagonist Comments
Nal: beta-(2-naphthyl)-D-alamine.
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
Phospholipase D stimulation
Other - See Comments
Comments:  BB3 receptor activates p125 focal adhesion kinase tyrosine phosphyloryation. Actvates protein kinase C and increases intracellular calcium.
References:  8,34,40-41,48
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
G protein (identity unknown) Other - See Comments
Comments:  Activation of tyrosine kinase cascades, MAPK , EGFR transactivation, CREB and MEK and ELK-1 have been associated with activation of BB3 receptor. In addition, activation of BB3 receptor stimulates p125 FAK, paxillin, MAPK and EGFR transactivation, involving activation of reactive oxygen species, matrix metalloproteinase and Src [28,34,48].
References: 
Tissue Distribution Click here for help
Germ cells in testis and lung carcinoma cells.
Species:  Human
Technique:  PCR/homology screening.
References:  5
Brain (paraventricular, arcuate, striohypothalamic, dorsal hypothalamic and dorsomedial hypothalamic nuclei, medial and lateral preoptic areas, and lateral and posterior hypothalamic areas).
Species:  Mouse
Technique:  Northern Blot and in situ hybridisation.
References:  32
Mapping in MOUSE and RAT brain. Highest in hypothamus (particularly preoptic nucleus, paraventricular, arcuate, and dorsomedial nuclei).
Species:  Mouse
Technique:  In situ hybridisation.
References:  51
Brain mapping: highest expression in hypothalamic nuclei, diagonal band, bed nucleus of strai terminalis, medial optic area, medial amygdaloid and parabrachial nuclei.
Species:  Mouse
Technique:  [3H]Bag-2 binding.
References:  12
Testis.
Species:  Rat
Technique:  Northern Blot and in situ hybridisation.
References:  5
Medial habenula nucleus, various hypothalamic nuclei, also cerebral cortex, hippocampus formation, thalmus and hypothamus.
Species:  Rat
Technique:  Immunohistochemistry, RT-PCR
References:  16,18
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Measurement of MAPK activation.
Species:  Human
Tissue:  Lung cancer cells or hBRS-3 (BB3)-transfected cell lines (Balb 3T3, NCI-H1299).
Response measured:  p42/p44 MAPK formation.
References:  3,28,49
Measurement of PLC activation and/or Ca2+ levels in lung cancer cells, as well as in a hBRS-3-transfected cell lines (Balb 3T3, NCI-H1299 cells).
Species:  Human
Tissue:  Transfected cells and human lung cancer cells.
Response measured:  [3H]IP generation, increase in cytosolic Ca2+.
References:  10,34,40,42,44
Measurement of PLC activity, PLD activity, and intracellular calcium mobilisation in NCI-N417 cells containing native human BB3 receptors.
Species:  Human
Tissue:  NCI-N417 human small cell lung carcinoma cells.
Response measured:  Stimulation of PLD activity.
Stimulation of PLC activity and subsequent intracellular calcium mobilisation.
References:  10,41,44,48
Physiological Functions Click here for help
Role in sperm cell division, maturation, or function. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Species:  Human
Tissue:  Germ cells in testis.
References:  5
Stimulates growth of both normal tissues and of BB3 receptor containing lung tumors
Species:  Human
Tissue:  Lung cancer cells and bronchial epithelial cells.
References:  28,45
Involved in body temperature regulation. BRS-3 agonists/BRS-3 knockout mice have altered body temperature.
Species:  Mouse
Tissue:  In vivo.
References:  13,26
Role in insulin secretion. Blockade of BB3 receptor or receptor knock-down with small interfering RNAs replicates the alteration in islet insulin release/regulation as observed in BB3 receptor knockout mice.
Species:  Mouse
Tissue:  In vivo and isolated pancreatic islet cells.
References:  6
Involved in the effect of insulin on skeletal muscle. In diabetics and obese patients BB3receptor is downregulated in skeletal muscle. Altered metabolic states have altered muscle BB3receptor stimulated glucose transport, GLUT-4 levels. BB3receptor mediated glucose transport is inhibited by wortmammin and PD98059.
Species:  Human
Tissue:  Myocytes.
References:  37
Involved in energy homeostasis. MK-5046, a BB3 receptor selective agonist causes weight loss similar to that observed in receptor knockout studies.
Species:  Mouse
Tissue:  In vivo.
References:  12-13
Physiological Consequences of Altering Gene Expression Click here for help
BB3 receptor knockout mice show mild late-onset obesity, hyperphagia and reduced metabolic rate.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  1,17
BB3 receptor knockout mice show impaired glucose metabolism possibly as a result of disruption of the GLUT4 translocation system in adipocytes.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  30
BB3 receptor knockout mice develope mild obesity, hypertension, and impaired glucose metabolism.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  33
BB3 receptor knockout mice display overexpression of MCH (melanin concentrating hormone) receptors. MCH treatment induces hyperleptinemia (leptin resistance) and feeding facilitation.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  20
BB3 receptor knockout mice show altered body temperature regulation.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  29
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Brs3tm1Jfb Brs3tm1Jfb/Brs3tm1Jfb
B6.129X1-Brs3		 MGI:1100501  MP:0006319 abnormal epididymal fat pad morphology PMID: 18039774 
Brs3tm1Jfb Brs3tm1Jfb/Brs3tm1Jfb
B6.129X1-Brs3		 MGI:1100501  MP:0005449 abnormal food intake PMID: 18039774 
Brs3tm1Hoh Brs3tm1Hoh/Brs3tm1Hoh
involves: 129P2/OlaHsd * C57BL/6J		 MGI:1100501  MP:0002078 abnormal glucose homeostasis PMID: 9367152 
Brs3tm1Hoh Brs3tm1Hoh/Brs3tm1Hoh
involves: 129P2/OlaHsd * C57BL/6J		 MGI:1100501  MP:0005120 decreased circulating growth hormone level PMID: 9367152 
Brs3tm1Hoh Brs3tm1Hoh/Brs3tm1Hoh
involves: 129P2/OlaHsd * C57BL/6J		 MGI:1100501  MP:0003912 decreased drinking behavior PMID: 9367152 
Brs3tm1Hoh Brs3tm1Hoh/Brs3tm1Hoh
involves: 129P2/OlaHsd * C57BL/6J		 MGI:1100501  MP:0005290 decreased oxygen consumption PMID: 9367152 
Brs3tm1Jfb Brs3tm1Jfb/Brs3tm1Jfb
B6.129X1-Brs3		 MGI:1100501  MP:0001260 increased body weight PMID: 18039774 
Brs3tm1Jfb Brs3tm1Jfb/Brs3tm1Jfb
B6.129X1-Brs3		 MGI:1100501  MP:0000005 increased brown adipose tissue amount PMID: 18039774 
Brs3tm1Hoh Brs3tm1Hoh/Brs3tm1Hoh
involves: 129P2/OlaHsd * C57BL/6J		 MGI:1100501  MP:0002079 increased circulating insulin level PMID: 9367152 
Brs3tm1Jfb Brs3tm1Jfb/Brs3tm1Jfb
B6.129X1-Brs3		 MGI:1100501  MP:0002079 increased circulating insulin level PMID: 18039774 
Brs3tm1Hoh Brs3tm1Hoh/Brs3tm1Hoh
involves: 129P2/OlaHsd * C57BL/6J		 MGI:1100501  MP:0005669 increased circulating leptin level PMID: 9367152 
Brs3tm1Jfb Brs3tm1Jfb/Brs3tm1Jfb
B6.129X1-Brs3		 MGI:1100501  MP:0005669 increased circulating leptin level PMID: 18039774 
Brs3tm1Jfb Brs3tm1Jfb/Brs3tm1Jfb
B6.129X1-Brs3		 MGI:1100501  MP:0003909 increased eating behavior PMID: 18039774 
Brs3tm1Hoh Brs3tm1Hoh/Brs3tm1Hoh
involves: 129P2/OlaHsd * C57BL/6J		 MGI:1100501  MP:0002842 increased systemic arterial blood pressure PMID: 9367152 
Brs3tm1Hoh Brs3tm1Hoh/Brs3tm1Hoh
involves: 129P2/OlaHsd * C57BL/6J		 MGI:1100501  MP:0000008 increased white adipose tissue amount PMID: 9367152 
Brs3tm1Jfb Brs3tm1Jfb/Brs3tm1Jfb
B6.129X1-Brs3		 MGI:1100501  MP:0000008 increased white adipose tissue amount PMID: 18039774 
Brs3tm1Hoh Brs3tm1Hoh/Brs3tm1Hoh
involves: 129P2/OlaHsd * C57BL/6J		 MGI:1100501  MP:0001261 obese PMID: 9367152 
Brs3tm1Hoh Brs3tm1Hoh/Brs3tm1Hoh
involves: 129P2/OlaHsd * C57BL/6J		 MGI:1100501  MP:0001433 polyphagia PMID: 9367152 
Biologically Significant Variants Click here for help
Type:  Missense mutation
Species:  Human
Description:  I606V non-synonymous variant may show a weak association with major depressive disorder (MDD) in females.
SNP accession:  rs13440581

References

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1. Aoki K, Sun YJ, Aoki S, Wada K, Wada E. (2002) Cloning, expression, and mapping of a gene that is upregulated in adipose tissue of mice deficient in bombesin receptor subtype-3. Biochem Biophys Res Commun, 290 (4): 1282-8. [PMID:11812002]

2. Boyle RG, Humphries J, Mitchell T, Showell GA, Apaya R, Iijima H, Shimada H, Arai T, Ueno H, Usui Y et al.. (2005) The design of a new potent and selective ligand for the orphan bombesin receptor subtype 3 (BRS3). J Pept Sci, 11 (3): 136-41. [PMID:15635635]

3. Cai H, Yang H, Xiang B, Li S, Liu S, Wan L, Zhang J, Li Y, Cheng J, Lu X. (2010) Selective apoptotic killing of solid and hematologic tumor cells by bombesin-targeted delivery of mitochondria-disrupting peptides. Mol Pharm, 7 (2): 586-96. [PMID:20141196]

4. Chobanian HR, Guo Y, Liu P, Chioda M, Lanza Jr TJ, Chang L, Kelly TM, Kan Y, Palyha O, Guan XM et al.. (2012) Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity. ACS Med Chem Lett, 3 (3): 252-6. [PMID:24900461]

5. Fathi Z, Corjay MH, Shapira H, Wada E, Benya R, Jensen R, Viallet J, Sausville EA, Battey JF. (1993) BRS-3: a novel bombesin receptor subtype selectively expressed in testis and lung carcinoma cells. J Biol Chem, 268 (8): 5979-84. [PMID:8383682]

6. Feng Y, Guan XM, Li J, Metzger JM, Zhu Y, Juhl K, Zhang BB, Thornberry NA, Reitman ML, Zhou YP. (2011) Bombesin receptor subtype-3 (BRS-3) regulates glucose-stimulated insulin secretion in pancreatic islets across multiple species. Endocrinology, 152 (11): 4106-15. [PMID:21878513]

7. Foster SR, Hauser AS, Vedel L, Strachan RT, Huang XP, Gavin AC, Shah SD, Nayak AP, Haugaard-Kedström LM, Penn RB et al.. (2019) Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors. Cell, 179 (4): 895-908.e21. [PMID:31675498]

8. Furutani N, Hondo M, Tsujino N, Sakurai T. (2010) Activation of bombesin receptor subtype-3 influences activity of orexin neurons by both direct and indirect pathways. J Mol Neurosci, 42 (1): 106-11. [PMID:20467915]

9. Gonzalez N, Hocart SJ, Portal-Nuñez S, Mantey SA, Nakagawa T, Zudaire E, Coy DH, Jensen RT. (2008) Molecular basis for agonist selectivity and activation of the orphan bombesin receptor subtype 3 receptor. J Pharmacol Exp Ther, 324 (2): 463-74. [PMID:18006692]

10. González N, Mantey SA, Pradhan TK, Sancho V, Moody TW, Coy DH, Jensen RT. (2009) Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors. Peptides, 30 (8): 1473-86. [PMID:19463875]

11. Gorbulev V, Akhundova A, Grzeschik KH, Fahrenholz F. (1994) Organization and chromosomal localization of the gene for the human bombesin receptor subtype expressed in pregnant uterus. FEBS Lett, 340 (3): 260-4. [PMID:8131855]

12. Guan XM, Chen H, Dobbelaar PH, Dong Y, Fong TM, Gagen K, Gorski J, He S, Howard AD, Jian T et al.. (2010) Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity. Cell Metab, 11 (2): 101-12. [PMID:20096642]

13. Guan XM, Metzger JM, Yang L, Raustad KA, Wang SP, Spann SK, Kosinski JA, Yu H, Shearman LP, Faidley TD et al.. (2011) Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist. J Pharmacol Exp Ther, 336 (2): 356-64. [PMID:21036912]

14. He S, Dobbelaar PH, Liu J, Jian T, Sebhat IK, Lin LS, Goodman A, Guo C, Guzzo PR, Hadden M et al.. (2010) Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists. Bioorg Med Chem Lett, 20 (6): 1913-7. [PMID:20167483]

15. Iwabuchi M, Ui-Tei K, Yamada K, Matsuda Y, Sakai Y, Tanaka K, 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 (3): 555-66. [PMID:12788815]

16. Jennings CA, Harrison DC, Maycox PR, Crook B, Smart D, Hervieu GJ. (2003) The distribution of the orphan bombesin receptor subtype-3 in the rat CNS. Neuroscience, 120 (2): 309-24. [PMID:12890504]

17. Ladenheim EE, Hamilton NL, Behles RR, Bi S, Hampton LL, Battey JF, Moran TH. (2008) Factors contributing to obesity in bombesin receptor subtype-3-deficient mice. Endocrinology, 149 (3): 971-8. [PMID:18039774]

18. Liu J, Lao ZJ, Zhang J, Schaeffer MT, Jiang MM, Guan XM, Van der Ploeg LH, Fong TM. (2002) Molecular basis of the pharmacological difference between rat and human bombesin receptor subtype-3 (BRS-3). Biochemistry, 41 (28): 8954-60. [PMID:12102638]

19. Liu P, Lanza Jr TJ, Chioda M, Jones C, Chobanian HR, Guo Y, Chang L, Kelly TM, Kan Y, Palyha O et al.. (2011) Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality. ACS Med Chem Lett, 2 (12): 933-7. [PMID:24900283]

20. Maekawa F, Quah HM, Tanaka K, Ohki-Hamazaki H. (2004) Leptin resistance and enhancement of feeding facilitation by melanin-concentrating hormone in mice lacking bombesin receptor subtype-3. Diabetes, 53 (3): 570-6. [PMID:14988239]

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