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

General Information of Drug (ID: DMEAOZ0)

Drug Name

Cilengitide Drug Info

Synonyms

Cilengitide; 188968-51-6; EMD-121974; Cilengitide [USAN:INN]; UNII-4EDF46E4GI; EMD121974; EMD-12192; EMD 121974; 4EDF46E4GI; CHEMBL429876; 2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid; Cyclo(L-arginylglycyl-L-aspartyl-D-phenylalanyl-N-methyl-L-valyl); Cyclo(L-arginylglycyl-L-alpha-aspartyl-D-phenylalanyl-N-methyl-L-valyl); Cilengitide (TFA salt)

Indication

Disease Entry	ICD 11	Status	REF
Rheumatoid arthritis	FA20	Phase 3	[1] , [2]

Cross-matching ID

PubChem CID: 176873
CAS Number: CAS 188968-51-6
TTD Drug ID: DMEAOZ0

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Integrin alpha-V/beta-3 (ITGAV/B3)	TT69TQN	ITAV_HUMAN-ITB3_HUMAN	Modulator	[3] , [4]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Integrin alpha-V/beta-3 (ITGAV/B3)	DTT	ITGAV-ITGB3	3.916	4.104	5.776	4.121

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Rheumatoid arthritis

ICD Disease Classification

FA20

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Integrin alpha-V/beta-3 (ITGAV/B3)	DTT	ITGAV-ITGB3	8.19E-02	-0.16	-0.46

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	URL: 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: 6597).
2	ClinicalTrials.gov (NCT00689221) Cilengitide, Temozolomide, and Radiation Therapy in Treating Patients With Newly Diagnosed Glioblastoma and Methylated Gene Promoter Status. U.S. National Institutes of Health.
3	The integrin antagonist cilengitide activates alphaVbeta3, disrupts VE-cadherin localization at cell junctions and enhances permeability in endothelial cells.PLoS One.2009;4(2):e4449.
4	Pharmacological inhibition of integrin alphavbeta3 aggravates experimental liver fibrosis and suppresses hepatic angiogenesis.Hepatology.2009 Nov;50(5):1501-11.