Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTQX45UM)

• DOT Name: G-protein coupled receptor 87 (GPR87)
• Synonyms: G-protein coupled receptor 95
• Gene Name: GPR87
• UniProt ID: GPR87_HUMAN
• Pfam ID: PF00001
• Sequence:
  MGFNLTLAKLPNNELHGQESHNSGNRSDGPGKNTTLHNEFDTIVLPVLYLIIFVASILLN
  GLAVWIFFHIRNKTSFIFYLKNIVVADLIMTLTFPFRIVHDAGFGPWYFKFILCRYTSVL
  FYANMYTSIVFLGLISIDRYLKVVKPFGDSRMYSITFTKVLSVCVWVIMAVLSLPNIILT
  NGQPTEDNIHDCSKLKSPLGVKWHTAVTYVNSCLFVAVLVILIGCYIAISRYIHKSSRQF
  ISQSSRKRKHNQSIRVVVAVFFTCFLPYHLCRIPFTFSHLDRLLDESAQKILYYCKEITL
  FLSACNVCLDPIIYFFMCRSFSRRLFKKSNIRTRSESIRSLQSVRRSEVRIYYDYTDV
• Function: Receptor for lysophosphatidic acid (LPA). Necessary for p53/TP53-dependent survival in response to DNA damage.
• Tissue Specificity: Expressed in placenta and prostate. Weaker expression in thymus. Not expressed in thalamus, hippocampus, pons or cerebellum. Overexpressed in squamous cell carcinoma of the lung.

Molecular Interaction Atlas (MIA) of This DOT

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate decreases the expression of G-protein coupled receptor 87 (GPR87).	[1]
Ciclosporin	DMAZJFX	Approved	Ciclosporin increases the expression of G-protein coupled receptor 87 (GPR87).	[2]
Tretinoin	DM49DUI	Approved	Tretinoin increases the expression of G-protein coupled receptor 87 (GPR87).	[3]
Acetaminophen	DMUIE76	Approved	Acetaminophen decreases the expression of G-protein coupled receptor 87 (GPR87).	[4]
Cisplatin	DMRHGI9	Approved	Cisplatin decreases the expression of G-protein coupled receptor 87 (GPR87).	[5]
Estradiol	DMUNTE3	Approved	Estradiol increases the expression of G-protein coupled receptor 87 (GPR87).	[6]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide increases the expression of G-protein coupled receptor 87 (GPR87).	[7]
Carbamazepine	DMZOLBI	Approved	Carbamazepine affects the expression of G-protein coupled receptor 87 (GPR87).	[8]
Fluorouracil	DMUM7HZ	Approved	Fluorouracil increases the expression of G-protein coupled receptor 87 (GPR87).	[9]
Cidofovir	DMA13GD	Approved	Cidofovir decreases the expression of G-protein coupled receptor 87 (GPR87).	[5]
Ifosfamide	DMCT3I8	Approved	Ifosfamide decreases the expression of G-protein coupled receptor 87 (GPR87).	[5]
Clodronate	DM9Y6X7	Approved	Clodronate decreases the expression of G-protein coupled receptor 87 (GPR87).	[5]
Adefovir dipivoxil	DMMAWY1	Approved	Adefovir dipivoxil increases the expression of G-protein coupled receptor 87 (GPR87).	[5]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of G-protein coupled receptor 87 (GPR87).	[11]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A increases the expression of G-protein coupled receptor 87 (GPR87).	[12]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde decreases the expression of G-protein coupled receptor 87 (GPR87).	[13]

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 decreases the methylation of G-protein coupled receptor 87 (GPR87).	[10]

References

• [1] From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
• [2] Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
• [3] Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
• [4] Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.
• [5] Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
• [6] Long-term estrogen exposure promotes carcinogen bioactivation, induces persistent changes in gene expression, and enhances the tumorigenicity of MCF-7 human breast cancer cells. Toxicol Appl Pharmacol. 2009 Nov 1;240(3):355-66.
• [7] Identification of transcriptome signatures and biomarkers specific for potential developmental toxicants inhibiting human neural crest cell migration. Arch Toxicol. 2016 Jan;90(1):159-80.
• [8] Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
• [9] Evaluation of developmental toxicity using undifferentiated human embryonic stem cells. J Appl Toxicol. 2015 Feb;35(2):205-18.
• [10] 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.
• [11] Inhibition of BRD4 attenuates tumor cell self-renewal and suppresses stem cell signaling in MYC driven medulloblastoma. Oncotarget. 2014 May 15;5(9):2355-71.
• [12] Transcriptomic?pathway?and?benchmark dose analysis of Bisphenol A, Bisphenol S, Bisphenol F, and 3,3',5,5'-Tetrabromobisphenol A in H9 human embryonic stem cells. Toxicol In Vitro. 2021 Apr;72:105097. doi: 10.1016/j.tiv.2021.105097. Epub 2021 Jan 18.
• [13] Regulation of chromatin assembly and cell transformation by formaldehyde exposure in human cells. Environ Health Perspect. 2017 Sep 21;125(9):097019.