Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTQ5FEI0)

• DOT Name: Phosphatidylethanolamine-binding protein 1 (PEBP1)
• Synonyms: PEBP-1; HCNPpp; Neuropolypeptide h3; Prostatic-binding protein; Raf kinase inhibitor protein; RKIP
• Gene Name: PEBP1
• UniProt ID: PEBP1_HUMAN
• PDB ID: 1BD9; 1BEH; 2L7W; 2QYQ
• Pfam ID: PF01161
• Sequence:
  MPVDLSKWSGPLSLQEVDEQPQHPLHVTYAGAAVDELGKVLTPTQVKNRPTSISWDGLDS
  GKLYTLVLTDPDAPSRKDPKYREWHHFLVVNMKGNDISSGTVLSDYVGSGPPKGTGLHRY
  VWLVYEQDRPLKCDEPILSNRSGDHRGKFKVASFRKKYELRAPVAGTCYQAEWDDYVPKL
  YEQLSGK
• Function: Binds ATP, opioids and phosphatidylethanolamine. Has lower affinity for phosphatidylinositol and phosphatidylcholine. Serine protease inhibitor which inhibits thrombin, neuropsin and chymotrypsin but not trypsin, tissue type plasminogen activator and elastase. Inhibits the kinase activity of RAF1 by inhibiting its activation and by dissociating the RAF1/MEK complex and acting as a competitive inhibitor of MEK phosphorylation; HCNP may be involved in the function of the presynaptic cholinergic neurons of the central nervous system. HCNP increases the production of choline acetyltransferase but not acetylcholinesterase. Seems to be mediated by a specific receptor.
• Reactome Pathway:
  Negative regulation of MAPK pathway (R-HSA-5675221)
  Signaling by moderate kinase activity BRAF mutants (R-HSA-6802946)
  Signaling by high-kinase activity BRAF mutants (R-HSA-6802948)
  Signaling by BRAF and RAF1 fusions (R-HSA-6802952)
  Paradoxical activation of RAF signaling by kinase inactive BRAF (R-HSA-6802955)
  Signaling downstream of RAS mutants (R-HSA-9649948)
  MAP2K and MAPK activation (R-HSA-5674135)

Molecular Interaction Atlas (MIA) of This DOT

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[1]
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[2]
Acetaminophen	DMUIE76	Approved	Acetaminophen decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[3]
Doxorubicin	DMVP5YE	Approved	Doxorubicin increases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[4]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[5]
Ivermectin	DMDBX5F	Approved	Ivermectin decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[6]
Quercetin	DM3NC4M	Approved	Quercetin increases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[7]
Vorinostat	DMWMPD4	Approved	Vorinostat decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[8]
Clozapine	DMFC71L	Approved	Clozapine decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[9]
Malathion	DMXZ84M	Approved	Malathion decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[10]
Cocaine	DMSOX7I	Approved	Cocaine affects the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[11]
Zidovudine	DM4KI7O	Approved	Zidovudine decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[12]
Benzatropine	DMF7EXL	Approved	Benzatropine decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[9]
Tocopherol	DMBIJZ6	Phase 2	Tocopherol increases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[14]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[18]
chloropicrin	DMSGBQA	Investigative	chloropicrin increases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[19]
Deguelin	DMXT7WG	Investigative	Deguelin decreases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[20]
D-glucose	DMMG2TO	Investigative	D-glucose increases the expression of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[21]

1 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Resveratrol	DM3RWXL	Phase 3	Resveratrol affects the secretion of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[13]

3 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
G1	DMTV42K	Phase 1/2	G1 decreases the phosphorylation of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[15]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the methylation of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[16]
PMID28870136-Compound-52	DMFDERP	Patented	PMID28870136-Compound-52 affects the phosphorylation of Phosphatidylethanolamine-binding protein 1 (PEBP1).	[17]

References

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