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Background of Bombesin Receptors
The bombesin receptors are G protein-coupled receptors. They are activated when bind to endogenous ligands, including gastrin-releasing peptide (GRP), neuromedin B (NMB), and GRP18-27 (neuromedin C). The corresponding receptors are divided into three subtypes, including the NMB receptor (BB1 receptor), GRP receptor (BB2 receptor), and an orphan receptor (BB3 receptor).
Fig.1. Proposed molecular mechanisms mediating GRPR regulation of brain function. (Roesler, 2012)
Distribution and Function of Bombesin Receptors
The bombesin receptors are broadly expressed throughout the central nervous system (CNS), gastrointestinal tract, and other organs, which are responsible for many physiological and pathologic processes, such as the modulation of sensory transmission, thermoregulation, feeding and pituitary, gastric, and pancreatic secretion, tissue development, as well as the regulation of lung cancer, eating disorder and obesity, CNS diseases, memory loss and behavior disorders, and inflammatory diseases.
Subtypes and Mechanisms of Bombesin Receptors
The family of bombesin receptors contains three subtypes of receptors, BB1 receptor, BB2 receptor, and BB3 receptor. They all promote signal transduction through the family of Gq/G11 proteins.
Receptor
|
Gene
|
Mechanism
|
Agonists
|
Antagonists
|
BB1 receptor
|
NMBR
|
-
BB1 receptor attaches to NMB, Gq/G11 protein promotes signal transduction
-
BB1 receptor activates protein kinase C by phospholipase C
|
-
NMB
-
bombesin
-
ranatensin
-
litorin
-
phyllolitorin
-
MK-5046
|
-
PD 165929
-
D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2
-
kuwanon H
-
PD 168368
-
PD 176252
|
BB2 receptor
|
GRPR
|
-
BB2 receptor couples to Gq/G11 protein to promote signal transduction
-
BB2 receptor stimulates phospholipase C, phospholipase A2, phospholipase D, and adenylyl cyclase
|
-
GRP
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bombesin
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ranatensin
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litorin
-
neuromedin C
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NMB
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phyllolitorin
-
MK-5046
|
-
PD 168368
-
PD 176252
-
bombesin
-
AM-37
-
BAY86-7548
-
bantag-1
|
BB3 receptor
|
BRS3
|
-
BB3 receptor couples to Gq/G11 protein to promote signal transduction
-
BB3 receptor stimulates phospholipase C and phospholipase D
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BB3 receptor activates p125 focal adhesion kinase tyrosine phosphyloryation
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BB3 receptor activates protein kinase C and increases intracellular calcium
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BB3 receptor activates tyrosine kinase cascades, MAPK, EGFR transactivation, CREB, MEK, and ELK-1
|
-
bag-2
-
MK-5046
-
bombesin
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compound 21b
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compound 9g
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phenylacetyl-Ala,DTrp-phenthylamide
|
-
bantag-1
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D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2
-
ML-18
|
Assay List of Bombesin Receptors
Creative Biolabs can provide a range of assays of bombesin receptors. You can choose the assay in the list or contact us for more information:
NMBR GRPR BRS3
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
Calcium Flux Assay
|
S01YF-0822-KX1290
|
Magic™ Human NMBR In Vitro Agonist & Antagonist Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-0822-KX1292
|
Magic™ Human NMBR In Vitro Agonist Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-0822-KX1295
|
Magic™ Human NMBR In Vitro Antagonist Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-0822-KX1298
|
Magic™ Human NMBR In Vitro PAM Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-1122-KX231
|
Magic™ Human NMBR In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
β-Arrestin Assay
|
S01YF-0822-KX1291
|
Magic™ Human NMBR In Vitro Agonist β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
S01YF-0822-KX1294
|
Magic™ Human NMBR In Vitro Antagonist β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
S01YF-0822-KX1297
|
Magic™ Human NMBR In Vitro PAM β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
Internalization Assay
|
S01YF-0822-KX1293
|
Magic™ Human NMBR In Vitro Agonist Internalization Assay
|
U2OS
|
Internalization Assay
|
|
S01YF-0822-KX1296
|
Magic™ Human NMBR In Vitro Antagonist Internalization Assay
|
U2OS
|
Internalization Assay
|
|
S01YF-0822-KX1299
|
Magic™ Human NMBR In Vitro PAM Internalization Assay
|
U2OS
|
Internalization Assay
|
|
Radioligand Binding Assay
|
S01YF-0722-KX317
|
Magic™ Human NMBR In Vitro Agonist Radioligand Binding Assay
|
|
Radioligand Binding Assay
|
|
S01YF-1122-KX232
|
Magic™ Human NMBR In Vitro Radioligand Binding Assay
|
CHO-K1
|
Radioligand Binding Assay
|
|
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
Calcium Flux Assay
|
S01YF-0822-KX1300
|
Magic™ Human GRPR In Vitro Agonist & Antagonist Calcium Flux Assay
|
HEK293
|
Calcium Flux Assay
|
|
S01YF-0822-KX1303
|
Magic™ Human GRPR In Vitro Agonist Calcium Flux Assay
|
U2OS
|
Calcium Flux Assay
|
|
S01YF-0822-KX1306
|
Magic™ Human GRPR In Vitro Antagonist Calcium Flux Assay
|
U2OS
|
Calcium Flux Assay
|
|
S01YF-0822-KX1309
|
Magic™ Human GRPR In Vitro PAM Calcium Flux Assay
|
U2OS
|
Calcium Flux Assay
|
|
S01YF-1122-KX233
|
Magic™ Human GRPR In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
β-Arrestin Assay
|
S01YF-0822-KX1302
|
Magic™ Human GRPR In Vitro Agonist β-Arrestin Assay
|
U2OS
|
β-Arrestin Assay
|
|
S01YF-0822-KX1305
|
Magic™ Human GRPR In Vitro Antagonist β-Arrestin Assay
|
U2OS
|
β-Arrestin Assay
|
|
S01YF-0822-KX1308
|
Magic™ Human GRPR In Vitro PAM β-Arrestin Assay
|
U2OS
|
β-Arrestin Assay
|
|
Internalization Assay
|
S01YF-0822-KX1301
|
Magic™ Human GRPR In Vitro Agonist Internalization Assay
|
U2OS
|
Internalization Assay
|
|
S01YF-0822-KX1304
|
Magic™ Human GRPR In Vitro Antagonist Internalization Assay
|
U2OS
|
Internalization Assay
|
|
S01YF-0822-KX1307
|
Magic™ Human GRPR In Vitro PAM Internalization Assay
|
U2OS
|
Internalization Assay
|
|
Radioligand Binding Assay
|
S01YF-0722-KX318
|
Magic™ Human GRPR In Vitro Agonist Radioligand Binding Assay
|
|
Radioligand Binding Assay
|
|
S01YF-1122-KX234
|
Magic™ Human GRPR In Vitro Radioligand Binding Assay
|
CHO-K1
|
Radioligand Binding Assay
|
|
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
Calcium Flux Assay
|
S01YF-0722-KX88
|
Magic™ Human BRS3 In Vitro Calcium Assay, HEK293-Ga15
|
HEK293-Ga15
|
Calcium Flux Assay
|
|
S01YF-0822-KX1310
|
Magic™ Human BRS3 In Vitro Agonist & Antagonist Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-0822-KX1312
|
Magic™ Human BRS3 In Vitro Agonist Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-0822-KX1314
|
Magic™ Human BRS3 In Vitro Antagonist Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-0822-KX1316
|
Magic™ Human BRS3 In Vitro PAM Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-1122-KX235
|
Magic™ Human BRS3 In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
S01YF-1122-KX237
|
Magic™ Mouse BRS3 In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
S01YF-1122-KX238
|
Magic™ Rat BRS3 In Vitro Calcium Flux Assay
|
CHO-K1-Gα16
|
Calcium Flux Assay
|
|
β-Arrestin Assay
|
S01YF-0822-KX1311
|
Magic™ Human BRS3 In Vitro Agonist β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
S01YF-0822-KX1313
|
Magic™ Human BRS3 In Vitro Antagonist β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
S01YF-0822-KX1315
|
Magic™ Human BRS3 In Vitro PAM β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
Radioligand Binding Assay
|
S01YF-0722-KX319
|
Magic™ Human BRS3 In Vitro Agonist Radioligand Binding Assay
|
|
Radioligand Binding Assay
|
|
S01YF-1122-KX236
|
Magic™ Human BRS3 In Vitro Radioligand Binding Assay
|
CHO-K1
|
Radioligand Binding Assay
|
|
Published Data
Paper Title
|
ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth
|
Journal
|
Peptides
|
Published
|
2015
|
Abstract
|
BB3 receptor is a G protein-coupled receptor (GPCR). The study aimed to find out specific agonists and antagonists of the BB3 receptor. PD168368 is a nonpeptide antagonist for the BB1 receptor whereas PD176252 is a nonpeptide antagonist for the BB2 receptor (GRPR) and BB1 receptor (NMBR). ML-18 is the S-enantiomer of the nonpeptide analogs of PD176252. The study used ML-18 to investigate the effect of this antagonist on BRS-3 in lung cancer cells.
|
Result
|
ML-18 inhibited specific (125)I-BA1 (DTyr-Gln-Trp-Ala-Val-βAla-His-Phe-Nle-NH2)BB(6-14) binding to NCI-H1299 lung cancer cells stably transfected with BRS-3 with IC50 values of 4.8. However, ML-18 has a lower affinity to the BB1 receptor and BB2 receptor with IC50 values of 16 and >100μM, respectively. The result also showed that ML-18 inhibited the ability of BA1 to elevate cytosolic Ca(2+) in a reversible manner using lung cancer cells loaded with FURA2-AM. In addition, the study has demonstrated that ML-18 inhibited the proliferation of lung cancer cells. As a nonpeptide BRS-3 antagonist, ML-18 is used as a model to increase potency and selectivity, according to the results.
Fig.2. The ability of ML-18 and EMY-98 to inhibit specific I-BA1 binding to BRS-3. (Moody, 2015)
|
References
-
Roesler, R.; Schwartsmann, G. Gastrin-releasing peptide receptors in the central nervous system: role in brain function and as a drug target. Frontiers in endocrinology. 2012, 3, 159.
-
Moody, T. W.; et al. ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides. 2015, 64: 55-61.
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