Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMUGO9M)

Drug Name

Ac-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2 Drug Info

Synonyms

CHEMBL274874; Ac-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2; Acetyl-GRP(20-27); BDBM50012306; ZINC169366208

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Gastrin-releasing peptide receptor (GRPR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ASP-7147	DMGDF2X	Irritable bowel syndrome	DD91.0	Phase 2	[2]
RC-3095	DMIG98L	Solid tumour/cancer	2A00-2F9Z	Phase 2	[3]
177Lu-labelled NeoBOMB1	DM2TSMD	Solid tumour/cancer	2A00-2F9Z	Phase 2	[4]
177-Lu-NeoB	DM6JLNT	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[4]
177Lu-AMBA	DMFG1YA	Breast cancer	2C60-2C65	Phase 1	[5]
BIM-26226	DM9F4LP	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[6]
kuwanon H	DMVQDNR	Discovery agent	N.A.	Investigative	[7]
bombesin	DMDFQ0Y	Discovery agent	N.A.	Investigative	[8]
PD 168368	DMFNQEA	Discovery agent	N.A.	Investigative	[9]
MK-5046	DMS7C6R	Discovery agent	N.A.	Investigative	[10]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Gastrin-releasing peptide receptor (GRPR)	TTC1MVT	GRPR_HUMAN	Inhibitor	[1]

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References

1	Gastrin releasing peptide antagonists with improved potency and stability. J Med Chem. 1991 Jul;34(7):2102-7.
2	Astellas and Drais Partner To Develop Third Astellas Compound through Tacurion
3	Lipid modification of GRN163, an N3'-->P5' thio-phosphoramidate oligonucleotide, enhances the potency of telomerase inhibition. Oncogene. 2005 Aug 4;24(33):5262-8.
4	68Ga/177Lu-NeoBOMB1, a Novel Radiolabeled GRPR Antagonist for Theranostic Use in Oncology. J Nucl Med. 2017 Feb;58(2):293-299.
5	Multimodality imaging and preclinical evaluation of 177Lu-AMBA for human prostate tumours in a murine model. Anticancer Res. 2010 Oct;30(10):4039-48.
6	Effect 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.
7	Non-peptide bombesin receptor antagonists, kuwanon G and H, isolated from mulberry. Biochem Biophys Res Commun. 1995 Aug 15;213(2):594-9.
8	Expression and characterization of cloned human bombesin receptors. Mol Pharmacol. 1995 Jan;47(1):10-20.
9	Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368. J Pharmacol Exp Ther. 1999 Sep;290(3):1202-11.
10	Comparative 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.