Target Information

Target General Infomation
Target ID
T68887
Former ID
TTDI01778
Target Name
Bombesin receptor
Gene Name
BRS3
Synonyms
BRS-3; Bombesin; Orphan receptor bombesin receptor subtype 3; BRS3
Target Type
Clinical Trial
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Function
Receptor for neuromedin-B.
BioChemical Class
GPCR rhodopsin
Target Validation
T01375
UniProt ID
P32247
Sequence
MAQRQPHSPNQTLISITNDTESSSSVVSNDNTNKGWSGDNSPGIEALCAIYITYAVIISV
GILGNAILIKVFFKTKSMQTVPNIFITSLAFGDLLLLLTCVPVDATHYLAEGWLFGRIGC
KVLSFIRLTSVGVSVFTLTILSADRYKAVVKPLERQPSNAILKTCVKAGCVWIVSMIFAL
PEAIFSNVYTFRDPNKNMTFESCTSYPVSKKLLQEIHSLLCFLVFYIIPLSIISVYYSLI
ARTLYKSTLNIPTEEQSHARKQIESRKRIARTVLVLVALFALCWLPNHLLYLYHSFTSQT
YVDPSAMHFIFTIFSRVLAFSNSCVNPFALYWLSKSFQKHFKAQLFCCKAERPEPPVADT
SLTTLAVMGTVPGTGSIQMSEISVTSFTGCSVKQAEDRF
Drugs and Mode of Action
Drug(s) BAY-86-7548 Drug Info Phase 1 Cancer [523178]
Demobesin Drug Info Phase 1 Breast cancer [522810]
Agonist bag-1 Drug Info [530652]
bag-2 Drug Info [530652]
bombesin Drug Info [533765]
compound 17c Drug Info [533071]
compound 21b Drug Info [535730]
compound 22e Drug Info [530736]
compound 8a Drug Info [532804]
compound 9f Drug Info [532620]
compound 9g Drug Info [532620]
MK-5046 Drug Info [531243]
neuromedin B Drug Info [533243]
phenylacetyl-Ala,DTrp-phenthylamide Drug Info [530886]
ranatensin Drug Info [525505]
[3H]bag-2 Drug Info [530652]
Antagonist bantag-1 Drug Info [532441]
Demobesin Drug Info [543802]
kuwanon H Drug Info [533672]
ML-18 Drug Info [533098]
PD 165929 Drug Info [543802]
PD 168368 Drug Info [530159]
PD 176252 Drug Info [530159]
Enhancer BAY-86-7548 Drug Info [532299]
Inhibitor [(N4-Bzdig)0]BB(7-14) Drug Info [527364]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Peptide GPCRs
References
Ref 522810ClinicalTrials.gov (NCT00989105) Technetium Tc 99m Demobesin-4 for Imaging Procedures in Patients With Prostate Cancer. U.S. National Institutes of Health.
Ref 523178ClinicalTrials.gov (NCT01205321) PET/CT Imaging for Radiation Dosimetry, Plasma Pharmacokinetics, Biodistribution, Safety and Tolerability and Diagnostic Performance of BAY86-7548 in Patients With Prostate Cancer and Healthy Volunteers. U.S. National Institutes of Health.
Ref 525505Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R). Biochemistry. 1999 Jun 1;38(22):7307-20.
Ref 527364J Med Chem. 2005 Jan 13;48(1):100-10.Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study.
Ref 530159Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors. Peptides. 2009 Aug;30(8):1473-86.
Ref 530652Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity. Cell Metab. 2010 Feb 3;11(2):101-12.
Ref 530736Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1913-7.
Ref 530886Pharmacology of putative selective hBRS-3 receptor agonists for human bombesin receptors (BnR): affinities, potencies and selectivity in multiple native and BnR transfected cells. Peptides. 2010 Aug;31(8):1569-78.
Ref 531243Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist. J Pharmacol Exp Ther. 2011 Feb;336(2):356-64.
Ref 532299Plasma pharmacokinetics, whole-body distribution, metabolism, and radiation dosimetry of 68Ga bombesin antagonist BAY 86-7548 in healthy men. J Nucl Med. 2013 Jun;54(6):867-72.
Ref 532441Comparative pharmacology of bombesin receptor subtype-3, nonpeptide agonist MK-5046, a universal peptide agonist, and peptide antagonist Bantag-1 for human bombesin receptors. J Pharmacol Exp Ther. 2013 Oct;347(1):100-16.
Ref 532620Discovery of novel chiral diazepines as bombesin receptor subtype-3 (BRS-3) agonists with low brain penetration. Bioorg Med Chem Lett. 2014 Feb 1;24(3):750-5.
Ref 532804Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality. ACS Med Chem Lett. 2011 Oct 3;2(12):933-7.
Ref 533071Synthesis and biological evaluation of novel chiral diazepine derivatives as bombesin receptor subtype-3 (BRS-3) agonists incorporating an antedrug approach. Bioorg Med Chem. 2015 Jan 1;23(1):89-104.
Ref 533098ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides. 2015 Feb;64:55-61.
Ref 533243Insights into bombesin receptors and ligands: Highlighting recent advances. Peptides. 2015 May 11. pii: S0196-9781(15)00145-X.
Ref 533672Non-peptide bombesin receptor antagonists, kuwanon G and H, isolated from mulberry. Biochem Biophys Res Commun. 1995 Aug 15;213(2):594-9.
Ref 533765Expression and characterization of cloned human bombesin receptors. Mol Pharmacol. 1995 Jan;47(1):10-20.
Ref 535730Design of selective peptidomimetic agonists for the human orphan receptor BRS-3. J Med Chem. 2003 May 8;46(10):1918-30.
Ref 543802(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 38).

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