Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT7WBSV)

• DTT Name: Oxoeicosanoid receptor 1 (OXER1)
• Synonyms: TG1019; GPR170; G-protein coupled receptor TG1019; G-protein coupled receptor R527; G-protein coupled receptor 170; 5-oxo-ETE G-protein coupled receptor
• Gene Name: OXER1
• DTT Type: Literature-reported target; [1]
• UniProt ID: OXER1_HUMAN
• TTD ID: T68834
• Sequence:
  MLCHRGGQLIVPIIPLCPEHSCRGRRLQNLLSGPWPKQPMELHNLSSPSPSLSSSVLPPS
  FSPSPSSAPSAFTTVGGSSGGPCHPTSSSLVSAFLAPILALEFVLGLVGNSLALFIFCIH
  TRPWTSNTVFLVSLVAADFLLISNLPLRVDYYLLHETWRFGAAACKVNLFMLSTNRTASV
  VFLTAIALNRYLKVVQPHHVLSRASVGAAARVAGGLWVGILLLNGHLLLSTFSGPSCLSY
  RVGTKPSASLRWHQALYLLEFFLPLALILFAIVSIGLTIRNRGLGGQAGPQRAMRVLAMV
  VAVYTICFLPSIIFGMASMVAFWLSACRSLDLCTQLFHGSLAFTYLNSVLDPVLYCFSSP
  NFLHQSRALLGLTRGRQGPVSDESSYQPSRQWRYREASRKAEAIGKLKVQGEVSLEKEGS
  SQG
• Function: Receptor for eicosanoids and polyunsaturated fatty acids such as 5-oxo-6E,8Z,11Z,14Z-eicosatetraenoic acid (5-OXO-ETE), 5(S)-hydroperoxy-6E,8Z,11Z,14Z-eicosatetraenoic acid (5(S)-HPETE) and arachidonic acid. Seems to be coupled to the G(i)/G(o), families of heteromeric G proteins.
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Eicosanoid ligand-binding receptors (R-HSA-391903)

Molecular Interaction Atlas (MIA) of This DTT

10 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
5-(6-chloro-2-hexyl-1H-indol-1-yl)-5-oxo-valeric acid	DM0K7U5	Discovery agent	N.A.	Investigative	[2]
5-oxo-12-HETE	DMLABR9	Discovery agent	N.A.	Investigative	[3]
5-oxo-15-HETE	DM9ZC7B	Discovery agent	N.A.	Investigative	[4]
5-oxo-20-HETE	DM493GU	Discovery agent	N.A.	Investigative	[4]
5-oxo-C20:3	DM6FSUW	Discovery agent	N.A.	Investigative	[5]
5-oxo-ODE	DM56TVA	Discovery agent	N.A.	Investigative	[6]
5S-HETE	DM3Z6G4	Discovery agent	N.A.	Investigative	[7]
5S-HPETE	DME1304	Discovery agent	N.A.	Investigative	[7]
Gue1654	DM89KNT	Discovery agent	N.A.	Investigative	[1]
[3H]5-oxo-ETE	DM50WFM	Discovery agent	N.A.	Investigative	[8]

References

• [1] A biased ligand for OXE-R uncouples Galpha and Gbetagamma signaling within a heterotrimer. Nat Chem Biol. 2012 Jul;8(7):631-8.
• [2] 5-Oxo-ETE receptor antagonists. J Med Chem. 2013 May 9;56(9):3725-32.
• [3] Biological inactivation of 5-oxo-6,8,11,14-eicosatetraenoic acid by human platelets. Blood. 1999 Feb 1;93(3):1086-96.
• [4] Metabolism and biologic effects of 5-oxoeicosanoids on human neutrophils. J Immunol. 1996 Jan 1;156(1):336-42.
• [5] Structural requirements for activation of the 5-oxo-6E,8Z, 11Z,14Z-eicosatetraenoic acid (5-oxo-ETE) receptor: identification of a mead acid metabolite with potent agonist activity. J Pharmacol Exp Ther. 2008 May;325(2):698-707.
• [6] Human neutrophils convert the sebum-derived polyunsaturated fatty acid Sebaleic acid to a potent granulocyte chemoattractant. J Biol Chem. 2008 Apr 25;283(17):11234-43.
• [7] TG1019/OXE, a Galpha(i/o)-protein-coupled receptor, mediates 5-oxo-eicosatetraenoic acid-induced chemotaxis. Biochem Biophys Res Commun. 2005 Sep 9;334(4):987-95.
• [8] Receptors for the 5-oxo class of eicosanoids in neutrophils. J Biol Chem. 1998 Dec 4;273(49):32535-41.