Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT978JZW)

• DOT Name: Prostaglandin E2 receptor EP1 subtype (PTGER1)
• Synonyms: PGE receptor EP1 subtype; PGE2 receptor EP1 subtype; Prostanoid EP1 receptor
• Gene Name: PTGER1
• UniProt ID: PE2R1_HUMAN
• Pfam ID: PF00001
• Sequence:
  MSPCGPLNLSLAGEATTCAAPWVPNTSAVPPSGASPALPIFSMTLGAVSNLLALALLAQA
  AGRLRRRRSAATFLLFVASLLATDLAGHVIPGALVLRLYTAGRAPAGGACHFLGGCMVFF
  GLCPLLLGCGMAVERCVGVTRPLLHAARVSVARARLALAAVAAVALAVALLPLARVGRYE
  LQYPGTWCFIGLGPPGGWRQALLAGLFASLGLVALLAALVCNTLSGLALLRARWRRRSRR
  PPPASGPDSRRRWGAHGPRSASASSASSIASASTFFGGSRSSGSARRARAHDVEMVGQLV
  GIMVVSCICWSPMLVLVALAVGGWSSTSLQRPLFLAVRLASWNQILDPWVYILLRQAVLR
  QLLRLLPPRAGAKGGPAGLGLTPSAWEASSLRSSRHSGLSHF
• Function: Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(q) proteins which activate a phosphatidylinositol-calcium second messenger system. May play a role as an important modulator of renal function. Implicated the smooth muscle contractile response to PGE2 in various tissues.
• Tissue Specificity: Abundant in kidney. Lower level expression in lung, skeletal muscle and spleen, lowest expression in testis and not detected in liver brain and heart.
• KEGG Pathway:
  Calcium sig.ling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Human cytomegalovirus infection (hsa05163)
  Pathways in cancer (hsa05200)
• Reactome Pathway:
  G alpha (q) signalling events (R-HSA-416476)
  Prostanoid ligand receptors (R-HSA-391908)

Molecular Interaction Atlas (MIA) of This DOT

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Resveratrol	DM3RWXL	Phase 3	Resveratrol decreases the expression of Prostaglandin E2 receptor EP1 subtype (PTGER1).	[1]
Epigallocatechin gallate	DMCGWBJ	Phase 3	Epigallocatechin gallate decreases the expression of Prostaglandin E2 receptor EP1 subtype (PTGER1).	[1]
Guaiacol	DMN4E7T	Phase 3	Guaiacol decreases the expression of Prostaglandin E2 receptor EP1 subtype (PTGER1).	[1]
Genistein	DM0JETC	Phase 2/3	Genistein decreases the expression of Prostaglandin E2 receptor EP1 subtype (PTGER1).	[1]
Puerarin	DMJIMXH	Phase 2	Puerarin decreases the expression of Prostaglandin E2 receptor EP1 subtype (PTGER1).	[1]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the methylation of Prostaglandin E2 receptor EP1 subtype (PTGER1).	[2]

References

• [1] Examining the genomic influence of skin antioxidants in vitro. Mediators Inflamm. 2010;2010.
• [2] Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.