Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT3R7HDZ)

• DOT Name: Gastric inhibitory polypeptide receptor (GIPR)
• Synonyms: GIP-R; Glucose-dependent insulinotropic polypeptide receptor
• Gene Name: GIPR
• UniProt ID: GIPR_HUMAN
• PDB ID: 2QKH; 4HJ0; 6DKJ; 7DTY; 7FIN; 7FIY; 7RA3; 7RBT; 7VAB; 8ITL; 8ITM
• Pfam ID: PF00002 ; PF02793
• Sequence:
  MTTSPILQLLLRLSLCGLLLQRAETGSKGQTAGELYQRWERYRRECQETLAAAEPPSGLA
  CNGSFDMYVCWDYAAPNATARASCPWYLPWHHHVAAGFVLRQCGSDGQWGLWRDHTQCEN
  PEKNEAFLDQRLILERLQVMYTVGYSLSLATLLLALLILSLFRRLHCTRNYIHINLFTSF
  MLRAAAILSRDRLLPRPGPYLGDQALALWNQALAACRTAQIVTQYCVGANYTWLLVEGVY
  LHSLLVLVGGSEEGHFRYYLLLGWGAPALFVIPWVIVRYLYENTQCWERNEVKAIWWIIR
  TPILMTILINFLIFIRILGILLSKLRTRQMRCRDYRLRLARSTLTLVPLLGVHEVVFAPV
  TEEQARGALRFAKLGFEIFLSSFQGFLVSVLYCFINKEVQSEIRRGWHHCRLRRSLGEEQ
  RQLPERAFRALPSGSGPGEVPTSRGLSSGTLPGPGNEASRELESYC
• Function: This is a receptor for GIP. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
• KEGG Pathway:
  cAMP sig.ling pathway (hsa04024)
  Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  Glucagon-type ligand receptors (R-HSA-420092)
  G alpha (s) signalling events (R-HSA-418555)

Molecular Interaction Atlas (MIA) of This DOT

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate decreases the methylation of Gastric inhibitory polypeptide receptor (GIPR).	[1]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Cisplatin	DMRHGI9	Approved	Cisplatin increases the expression of Gastric inhibitory polypeptide receptor (GIPR).	[2]
Triclosan	DMZUR4N	Approved	Triclosan decreases the expression of Gastric inhibitory polypeptide receptor (GIPR).	[3]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the expression of Gastric inhibitory polypeptide receptor (GIPR).	[4]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of Gastric inhibitory polypeptide receptor (GIPR).	[5]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A affects the expression of Gastric inhibitory polypeptide receptor (GIPR).	[6]

References

• [1] Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
• [2] Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
• [3] Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
• [4] Identification of a transcriptomic signature of food-relevant genotoxins in human HepaRG hepatocarcinoma cells. Food Chem Toxicol. 2020 Jun;140:111297. doi: 10.1016/j.fct.2020.111297. Epub 2020 Mar 28.
• [5] Cell-based two-dimensional morphological assessment system to predict cancer drug-induced cardiotoxicity using human induced pluripotent stem cell-derived cardiomyocytes. Toxicol Appl Pharmacol. 2019 Nov 15;383:114761. doi: 10.1016/j.taap.2019.114761. Epub 2019 Sep 15.
• [6] A trichostatin A expression signature identified by TempO-Seq targeted whole transcriptome profiling. PLoS One. 2017 May 25;12(5):e0178302. doi: 10.1371/journal.pone.0178302. eCollection 2017.