Target Information

Target General Infomation
Target ID
T99816
Former ID
TTDC00230
Target Name
Gastrin-releasing peptide receptor
Gene Name
GRPR
Synonyms
Bombesin/gastrin-releasing peptide receptor; GRP-R; GRP-preferring bombesin receptor; GRPR
Target Type
Clinical Trial
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Receptor for gastrin releasing peptide (GRP). This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
BioChemical Class
GPCR rhodopsin
Target Validation
T99816
UniProt ID
P30550
Sequence
MALNDCFLLNLEVDHFMHCNISSHSADLPVNDDWSHPGILYVIPAVYGVIILIGLIGNIT
LIKIFCTVKSMRNVPNLFISSLALGDLLLLITCAPVDASRYLADRWLFGRIGCKLIPFIQ
LTSVGVSVFTLTALSADRYKAIVRPMDIQASHALMKICLKAAFIWIISMLLAIPEAVFSD
LHPFHEESTNQTFISCAPYPHSNELHPKIHSMASFLVFYVIPLSIISVYYYFIAKNLIQS
AYNLPVEGNIHVKKQIESRKRLAKTVLVFVGLFAFCWLPNHVIYLYRSYHYSEVDTSMLH
FVTSICARLLAFTNSCVNPFALYLLSKSFRKQFNTQLLCCQPGLIIRSHSTGRSTTCMTS
LKSTNPSVATFSLINGNICHERYV
Drugs and Mode of Action
Drug(s) ASP-7147 Drug Info Phase 2 Irritable bowel syndrome [524356]
RC-3095 Drug Info Phase 2 Solid tumours [531638], [531750], [541360]
177Lu-AMBA Drug Info Phase 1 Breast cancer [548826]
BIM-26226 Drug Info Discontinued in Phase 1 Cancer [545685]
Inhibitor (CH3)CCO-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2 Drug Info [531063]
(D)Phe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH2 Drug Info [525815]
Ac-His-Trp-Ala-Val-Ala-His-Leu-Met-NH2 Drug Info [531063]
Ac-His-Trp-Ala-Val-D-Ala-His-Leu-Met-NH2 Drug Info [531063]
Ac-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2 Drug Info [531063]
JMV 1535 Drug Info [525815]
JMV 1693 Drug Info [525815]
JMV 1719 Drug Info [525815]
JMV 1799 Drug Info [525815]
JMV 1801 Drug Info [525815]
JMV 1802 Drug Info [525815]
JMV 1803 Drug Info [525815]
JMV 1813 Drug Info [525815]
RC-3095 Drug Info [527581]
[(N4-Bzdig)0,Nle14]BB(7-14) Drug Info [527364]
[(N4-Bzdig)0]BB(7-14) Drug Info [527364]
[N40,Pro1,Tyr4,Nle 14]BB Drug Info [527364]
[N40,Pro1,Tyr4]BB Drug Info [527364]
[Tyr4]Bombesin Drug Info [527364]
Agonist 177Lu-AMBA Drug Info [531242]
bombesin Drug Info [533765]
MK-5046 Drug Info [532441]
neuromedin B Drug Info [533765]
ranatensin Drug Info [525505]
Antagonist ASP-7147 Drug Info [550285]
bantag-1 Drug Info [532441]
kuwanon H Drug Info [533672]
PD 168368 Drug Info [525567]
PD 176252 Drug Info [534800]
Modulator BIM-26226 Drug Info [534659]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Peptide GPCRs
GPCRs, Other
References
Ref 524356ClinicalTrials.gov (NCT01896583) A Phase 2 Pilot Study to Assess ASP7147 in Patients With Diarrhea Predominant Irritable Bowel Syndrome (IBS-D). U.S. National Institutes of Health.
Ref 531638Protective effect of RC-3095, an antagonist of the gastrin-releasing peptide receptor, in experimental arthritis. Arthritis Rheum. 2011 Oct;63(10):2956-65.
Ref 531750Gastrin-releasing peptide receptor (GRPR) mediates chemotaxis in neutrophils. Proc Natl Acad Sci U S A. 2012 Jan 10;109(2):547-52.
Ref 541360(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. (Ligand id: 6183).
Ref 545685Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004166)
Ref 548826Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029232)
Ref 525505Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R). Biochemistry. 1999 Jun 1;38(22):7307-20.
Ref 525567Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368. J Pharmacol Exp Ther. 1999 Sep;290(3):1202-11.
Ref 525815J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues.
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 527581Oncogene. 2005 Aug 4;24(33):5262-8.Lipid modification of GRN163, an N3'-->P5' thio-phosphoramidate oligonucleotide, enhances the potency of telomerase inhibition.
Ref 531063J Med Chem. 1991 Jul;34(7):2102-7.Gastrin releasing peptide antagonists with improved potency and stability.
Ref 531242Multimodality imaging and preclinical evaluation of 177Lu-AMBA for human prostate tumours in a murine model. Anticancer Res. 2010 Oct;30(10):4039-48.
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 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 534659Effect of the gastrin-releasing peptide antagonist BIM 26226 and lanreotide on an acinar pancreatic carcinoma. Eur J Pharmacol. 1998 Apr 17;347(1):77-86.
Ref 534800PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94.
Ref 550285Astellas and Drais Partner To Develop Third Astellas Compound through Tacurion

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