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

General Information of Drug (ID: DM1DMR2)

• Drug Name: C[RGDf-(3R)-Carboxymorpholine] Drug Info
• Synonyms: CHEMBL443362; c[RGDf-(3R)-Carboxymorpholine]

Indication

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

• Cross-matching ID:
  PubChem CID: 44123805
  TTD Drug ID: DM1DMR2

Molecule-Related Drug Atlas

Drug(s) Targeting Integrin alpha-V (ITGAV)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Abituzumab	DMTCXSG	Colorectal cancer	2B91.Z	Phase 2	[2]
IMGN-388	DMSYB83	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
SB-223245	DM3JQCF	N. A.	N. A.	Terminated	[4]
C(-GRGDfL-)	DMTMJAI	Discovery agent	N.A.	Investigative	[5]
SB-265123	DM8UKH7	Discovery agent	N.A.	Investigative	[6]
C(RGDfF)	DMMBESU	Discovery agent	N.A.	Investigative	[7]
Ac-Asp-Arg-Leu-Asp-Ser-OH	DMYHADT	Discovery agent	N.A.	Investigative	[8]
C[-Arg-Gly-Asp-Acpca21-]	DMXCUDV	Discovery agent	N.A.	Investigative	[9]
C-[-Arg-Gly-Asp-Acpca32-]	DMVM7B2	Discovery agent	N.A.	Investigative	[9]
Cyclo-[-Arg-Gly-Asp-Amp22-]	DMBELJK	Discovery agent	N.A.	Investigative	[10]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Integrin alpha-V (ITGAV)	TTT1R2L	ITAV_HUMAN	Inhibitor	[1]

References

• [1] Morpholine-based RGD-cyclopentapeptides as alphavbeta3/alphavbeta5 integrin ligands: role of configuration towards receptor binding affinity. Bioorg Med Chem. 2009 Feb 15;17(4):1542-9.
• [2] Abituzumab combined with cetuximab plus irinotecan versus cetuximab plus irinotecan alone for patients with KRAS wild-type metastatic colorectal cancer: the randomised phase I/II POSEIDON trial. Ann Oncol. 2015 Jan;26(1):132-40.
• [3] Anti-alphav integrin monoclonal antibody intetumumab enhances the efficacy of radiation therapy and reduces metastasis of human cancer xenografts in nude rats. Cancer Res. 2010 Oct 1;70(19):7591-9.
• [4] Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a resten... Bioorg Med Chem Lett. 1998 Nov 17;8(22):3171-6.
• [5] Multiple N-methylation by a designed approach enhances receptor selectivity. J Med Chem. 2007 Nov 29;50(24):5878-81.
• [6] 1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability. Bioorg Med Chem Lett. 2004 Dec 6;14(23):5937-41.
• [7] Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study ... J Med Chem. 2006 Mar 9;49(5):1808-17.
• [8] Synthesis and biological evaluation of non-peptide alpha(v)beta(3)/alpha(5)beta(1) integrin dual antagonists containing 5,6-dihydropyridin-2-one sc... Bioorg Med Chem. 2007 Dec 1;15(23):7380-90.
• [9] Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders. J Med Chem. 2005 Dec 1;48(24):7675-87.
• [10] Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues. J Med Chem. 2008 Mar 27;51(6):1771-82.