Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTEWWMB5)

• DOT Name: Olfactory receptor 51E2 (OR51E2)
• Synonyms: HPRAJ; Olfactory receptor OR11-16; Prostate-specific G-protein coupled receptor
• Gene Name: OR51E2
• UniProt ID: O51E2_HUMAN
• PDB ID: 8F76
• Pfam ID: PF13853
• Sequence:
  MSSCNFTHATFVLIGIPGLEKAHFWVGFPLLSMYVVAMFGNCIVVFIVRTERSLHAPMYL
  FLCMLAAIDLALSTSTMPKILALFWFDSREISFEACLTQMFFIHALSAIESTILLAMAFD
  RYVAICHPLRHAAVLNNTVTAQIGIVAVVRGSLFFFPLPLLIKRLAFCHSNVLSHSYCVH
  QDVMKLAYADTLPNVVYGLTAILLVMGVDVMFISLSYFLIIRTVLQLPSKSERAKAFGTC
  VSHIGVVLAFYVPLIGLSVVHRFGNSLHPIVRVVMGDIYLLLPPVINPIIYGAKTKQIRT
  RVLAMFKISCDKDLQAVGGK
• Function: Olfactory receptor. Activated by the odorant, beta-ionone, a synthetic terpenoid. The activity of this receptor is probably mediated by G-proteins leading to the elevation of intracellular Ca(2+), cAMP and activation of the protein kinases PKA and MAPK3/MAPK1. Stimulation of OR51E2 by beta-ionone affects melanocyte proliferation, differentiation, and melanogenesis. Activation of OR51E2 by beta-ionone increases proliferation and migration of primary retinal pigment epithelial (RPE) cells. Activated also by the short-chain fatty acids (SCFA) acetate and propionate. In response to SCFA, may positively regulate renin secretion and increase blood pressure. May also be activated by steroid hormones and regulate cell proliferation. Activated by L-lactate in glomus cells.
• Tissue Specificity: Highly expressed in the prostate . Also expressed in spleen, liver, olfactory epithelium, retinal pigment epithelium and medulla oblongata . In the retinal pigment epithelium expression is restricted to the pigment cells and choroid (at protein level) . Expressed in epidermal melanocytes (at protein level) .
• KEGG Pathway: Olfactory transduction (hsa04740)
• Reactome Pathway:
  Expression and translocation of olfactory receptors (R-HSA-9752946)
  Olfactory Signaling Pathway (R-HSA-381753)

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
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene affects the methylation of Olfactory receptor 51E2 (OR51E2).	[1]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Taurine	DMVW7N3	Investigative	Taurine decreases the expression of Olfactory receptor 51E2 (OR51E2).	[2]

References

• [1] 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.
• [2] Taurine-responsive genes related to signal transduction as identified by cDNA microarray analyses of HepG2 cells. J Med Food. 2006 Spring;9(1):33-41. doi: 10.1089/jmf.2006.9.33.