Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT4WVWBO)

• DOT Name: Proteinase-activated receptor 1 (F2R)
• Synonyms: PAR-1; Coagulation factor II receptor; Thrombin receptor
• Gene Name: F2R
• UniProt ID: PAR1_HUMAN
• PDB ID: 1NRN; 1NRO; 1NRP; 1NRQ; 1NRR; 3BEF; 3HKI; 3HKJ; 3LU9; 3VW7
• Pfam ID: PF00001
• Sequence:
  MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPRSFLLRNPNDKYEPFWEDEE
  KNESGLTEYRLVSINKSSPLQKQLPAFISEDASGYLTSSWLTLFVPSVYTGVFVVSLPLN
  IMAIVVFILKMKVKKPAVVYMLHLATADVLFVSVLPFKISYYFSGSDWQFGSELCRFVTA
  AFYCNMYASILLMTVISIDRFLAVVYPMQSLSWRTLGRASFTCLAIWALAIAGVVPLLLK
  EQTIQVPGLNITTCHDVLNETLLEGYYAYYFSAFSAVFFFVPLIISTVCYVSIIRCLSSS
  AVANRSKKSRALFLSAAVFCIFIICFGPTNVLLIAHYSFLSHTSTTEAAYFAYLLCVCVS
  SISCCIDPLIYYYASSECQRYVYSILCCKESSDPSSYNSSGQLMASKMDTCSSNLNNSIY
  KKLLT
• Function: High affinity receptor for activated thrombin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation and in vascular development.
• Tissue Specificity: Platelets and vascular endothelial cells.
• KEGG Pathway:
  Rap1 sig.ling pathway (hsa04015)
  Calcium sig.ling pathway (hsa04020)
  cAMP sig.ling pathway (hsa04024)
  Phospholipase D sig.ling pathway (hsa04072)
  Neuroactive ligand-receptor interaction (hsa04080)
  PI3K-Akt sig.ling pathway (hsa04151)
  Complement and coagulation cascades (hsa04610)
  Platelet activation (hsa04611)
  Regulation of actin cytoskeleton (hsa04810)
  Pathogenic Escherichia coli infection (hsa05130)
  Pathways in cancer (hsa05200)
• Reactome Pathway:
  Peptide ligand-binding receptors (R-HSA-375276)
  G alpha (q) signalling events (R-HSA-416476)
  Thrombin signalling through proteinase activated receptors (PARs) (R-HSA-456926)
  Common Pathway of Fibrin Clot Formation (R-HSA-140875)

Molecular Interaction Atlas (MIA) of This DOT

This DOT Affected the Drug Response of 4 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Etoposide	DMNH3PG	Approved	Proteinase-activated receptor 1 (F2R) affects the response to substance of Etoposide.	[29]
Mitomycin	DMH0ZJE	Approved	Proteinase-activated receptor 1 (F2R) affects the response to substance of Mitomycin.	[29]
Docetaxel	DMDI269	Approved	Proteinase-activated receptor 1 (F2R) decreases the response to substance of Docetaxel.	[30]
Clopidogrel	DMOL54H	Approved	Proteinase-activated receptor 1 (F2R) affects the response to substance of Clopidogrel.	[31]

34 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate increases the expression of Proteinase-activated receptor 1 (F2R).	[1]
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Proteinase-activated receptor 1 (F2R).	[2]
Doxorubicin	DMVP5YE	Approved	Doxorubicin increases the expression of Proteinase-activated receptor 1 (F2R).	[3]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate increases the expression of Proteinase-activated receptor 1 (F2R).	[4]
Arsenic	DMTL2Y1	Approved	Arsenic affects the expression of Proteinase-activated receptor 1 (F2R).	[5]
Quercetin	DM3NC4M	Approved	Quercetin increases the expression of Proteinase-activated receptor 1 (F2R).	[6]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide increases the expression of Proteinase-activated receptor 1 (F2R).	[7]
Hydrogen peroxide	DM1NG5W	Approved	Hydrogen peroxide increases the expression of Proteinase-activated receptor 1 (F2R).	[8]
Decitabine	DMQL8XJ	Approved	Decitabine increases the expression of Proteinase-activated receptor 1 (F2R).	[9]
Selenium	DM25CGV	Approved	Selenium decreases the expression of Proteinase-activated receptor 1 (F2R).	[10]
Fulvestrant	DM0YZC6	Approved	Fulvestrant increases the expression of Proteinase-activated receptor 1 (F2R).	[11]
Dexamethasone	DMMWZET	Approved	Dexamethasone increases the expression of Proteinase-activated receptor 1 (F2R).	[12]
Hydroquinone	DM6AVR4	Approved	Hydroquinone decreases the expression of Proteinase-activated receptor 1 (F2R).	[13]
Aspirin	DM672AH	Approved	Aspirin decreases the expression of Proteinase-activated receptor 1 (F2R).	[14]
Thalidomide	DM70BU5	Approved	Thalidomide decreases the expression of Proteinase-activated receptor 1 (F2R).	[15]
Vitamin B3	DMQVRZH	Approved	Vitamin B3 increases the expression of Proteinase-activated receptor 1 (F2R).	[16]
Lenalidomide	DM6Q7U4	Approved	Lenalidomide decreases the expression of Proteinase-activated receptor 1 (F2R).	[15]
Asasantin	DMCZIHT	Approved	Asasantin decreases the expression of Proteinase-activated receptor 1 (F2R).	[17]
Bivalirudin	DMECRX1	Approved	Bivalirudin decreases the activity of Proteinase-activated receptor 1 (F2R).	[18]
Tocopherol	DMBIJZ6	Phase 2	Tocopherol decreases the expression of Proteinase-activated receptor 1 (F2R).	[10]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the expression of Proteinase-activated receptor 1 (F2R).	[2]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of Proteinase-activated receptor 1 (F2R).	[19]
Scriptaid	DM9JZ21	Preclinical	Scriptaid affects the expression of Proteinase-activated receptor 1 (F2R).	[20]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A increases the expression of Proteinase-activated receptor 1 (F2R).	[1]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde increases the expression of Proteinase-activated receptor 1 (F2R).	[21]
Milchsaure	DM462BT	Investigative	Milchsaure increases the expression of Proteinase-activated receptor 1 (F2R).	[22]
Coumestrol	DM40TBU	Investigative	Coumestrol decreases the expression of Proteinase-activated receptor 1 (F2R).	[23]
chloropicrin	DMSGBQA	Investigative	chloropicrin increases the expression of Proteinase-activated receptor 1 (F2R).	[24]
methyl p-hydroxybenzoate	DMO58UW	Investigative	methyl p-hydroxybenzoate decreases the expression of Proteinase-activated receptor 1 (F2R).	[25]
D-glucose	DMMG2TO	Investigative	D-glucose decreases the expression of Proteinase-activated receptor 1 (F2R).	[26]
Phencyclidine	DMQBEYX	Investigative	Phencyclidine increases the expression of Proteinase-activated receptor 1 (F2R).	[27]
4-hydroxy-2-nonenal	DM2LJFZ	Investigative	4-hydroxy-2-nonenal decreases the expression of Proteinase-activated receptor 1 (F2R).	[8]
2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE	DMNQL17	Investigative	2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE decreases the expression of Proteinase-activated receptor 1 (F2R).	[28]
GW7604	DMCA4RM	Investigative	GW7604 increases the expression of Proteinase-activated receptor 1 (F2R).	[11]

References

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