Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT2D4V93)

• DOT Name: 2-oxoglutarate receptor 1 (OXGR1)
• Synonyms: Alpha-ketoglutarate receptor 1; G-protein coupled receptor 80; G-protein coupled receptor 99; P2Y purinoceptor 15; P2Y15; P2Y-like GPCR; P2Y-like nucleotide receptor
• Gene Name: OXGR1
• UniProt ID: OXGR1_HUMAN
• Pfam ID: PF00001
• Sequence:
  MNEPLDYLANASDFPDYAAAFGNCTDENIPLKMHYLPVIYGIIFLVGFPGNAVVISTYIF
  KMRPWKSSTIIMLNLACTDLLYLTSLPFLIHYYASGENWIFGDFMCKFIRFSFHFNLYSS
  ILFLTCFSIFRYCVIIHPMSCFSIHKTRCAVVACAVVWIISLVAVIPMTFLITSTNRTNR
  SACLDLTSSDELNTIKWYNLILTATTFCLPLVIVTLCYTTIIHTLTHGLQTDSCLKQKAR
  RLTILLLLAFYVCFLPFHILRVIRIESRLLSISCSIENQIHEAYIVSRPLAALNTFGNLL
  LYVVVSDNFQQAVCSTVRCKVSGNLEQAKKISYSNNP
• Function: Receptor for alpha-ketoglutarate. Seems to act exclusively through a G(q)-mediated pathway.
• Tissue Specificity: Detected in kidney and, to a lower extent, in placenta. Not detected in brain tissues including the frontal cortex, caudate putamen, thalamus, hypothalamus, hippocampus or pons.
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Class A/1 (Rhodopsin-like receptors) (R-HSA-373076)

Molecular Interaction Atlas (MIA) of This DOT

2 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 2-oxoglutarate receptor 1 (OXGR1).	[1]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the methylation of 2-oxoglutarate receptor 1 (OXGR1).	[4]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of 2-oxoglutarate receptor 1 (OXGR1).	[2]
Methotrexate	DM2TEOL	Approved	Methotrexate increases the expression of 2-oxoglutarate receptor 1 (OXGR1).	[3]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of 2-oxoglutarate receptor 1 (OXGR1).	[5]

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] Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
• [3] Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
• [4] 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.
• [5] CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer. J Clin Invest. 2016 Feb;126(2):639-52.