General Information of Drug Off-Target (DOT) (ID: OTCSMVF1)

DOT Name Prostaglandin D2 receptor 2 (PTGDR2)
Synonyms Chemoattractant receptor-homologous molecule expressed on Th2 cells; G-protein coupled receptor 44; CD antigen CD294
Gene Name PTGDR2
UniProt ID
PD2R2_HUMAN
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
PDB ID
6D26; 6D27; 7M8W
Pfam ID
PF00001
Sequence
MSANATLKPLCPILEQMSRLQSHSNTSIRYIDHAAVLLHGLASLLGLVENGVILFVVGCR
MRQTVVTTWVLHLALSDLLASASLPFFTYFLAVGHSWELGTTFCKLHSSIFFLNMFASGF
LLSAISLDRCLQVVRPVWAQNHRTVAAAHKVCLVLWALAVLNTVPYFVFRDTISRLDGRI
MCYYNVLLLNPGPDRDATCNSRQVALAVSKFLLAFLVPLAIIASSHAAVSLRLQHRGRRR
PGRFVRLVAAVVAAFALCWGPYHVFSLLEARAHANPGLRPLVWRGLPFVTSLAFFNSVAN
PVLYVLTCPDMLRKLRRSLRTVLESVLVDDSELGGAGSSRRRRTSSTARSASPLALCSRP
EEPRGPARLLGWLLGSCAASPQTGPLNRALSSTSS
Function
Receptor for prostaglandin D2 (PGD2). Coupled to the G(i)-protein. Receptor activation may result in pertussis toxin-sensitive decreases in cAMP levels and Ca(2+) mobilization. PI3K signaling is also implicated in mediating PTGDR2 effects. PGD2 induced receptor internalization. CRTH2 internalization can be regulated by diverse kinases such as, PKC, PKA, GRK2, GPRK5/GRK5 and GRK6. Receptor activation is responsible, at least in part, in immune regulation and allergic/inflammation responses.
Tissue Specificity
Widespread expression. High expression in stomach, small intestine, heart and thymus. Intermediate expression in colon, spinal cord and peripheral blood and low expression in brain, skeletal muscle and spleen. Expressed also on Th2- and Tc2- type cells, eosinophils and basophils.
Reactome Pathway
G alpha (i) signalling events (R-HSA-418594 )
Prostanoid ligand receptors (R-HSA-391908 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 1 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Aspirin DM672AH Approved Prostaglandin D2 receptor 2 (PTGDR2) affects the response to substance of Aspirin. [9]
------------------------------------------------------------------------------------
7 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 Prostaglandin D2 receptor 2 (PTGDR2). [1]
Arsenic DMTL2Y1 Approved Arsenic affects the expression of Prostaglandin D2 receptor 2 (PTGDR2). [2]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide increases the expression of Prostaglandin D2 receptor 2 (PTGDR2). [3]
Indomethacin DMSC4A7 Approved Indomethacin increases the activity of Prostaglandin D2 receptor 2 (PTGDR2). [4]
Urethane DM7NSI0 Phase 4 Urethane decreases the expression of Prostaglandin D2 receptor 2 (PTGDR2). [5]
Leflunomide DMR8ONJ Phase 1 Trial Leflunomide increases the expression of Prostaglandin D2 receptor 2 (PTGDR2). [7]
QUERCITRIN DM1DH96 Investigative QUERCITRIN increases the expression of Prostaglandin D2 receptor 2 (PTGDR2). [8]
------------------------------------------------------------------------------------
⏷ Show the Full List of 7 Drug(s)
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 D2 receptor 2 (PTGDR2). [6]
------------------------------------------------------------------------------------

References

1 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
2 Prenatal arsenic exposure and shifts in the newborn proteome: interindividual differences in tumor necrosis factor (TNF)-responsive signaling. Toxicol Sci. 2014 Jun;139(2):328-37. doi: 10.1093/toxsci/kfu053. Epub 2014 Mar 27.
3 Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.
4 Cutting edge: agonistic effect of indomethacin on a prostaglandin D2 receptor, CRTH2. J Immunol. 2002 Feb 1;168(3):981-5. doi: 10.4049/jimmunol.168.3.981.
5 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
6 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.
7 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
8 Molecular mechanisms of quercitrin-induced apoptosis in non-small cell lung cancer. Arch Med Res. 2014 Aug;45(6):445-54.
9 Genetic and ethnic risk factors associated with drug hypersensitivity. Curr Opin Allergy Clin Immunol. 2010 Aug;10(4):280-90. doi: 10.1097/ACI.0b013e32833b1eb3.